Current scenario of quinolone hybrids with potential antibacterial activity against ESKAPE pathogens

Article Biochemistry & Molecular Biology

Synthesis and molecular docking of new N4-piperazinyl ciprofloxacin hybrids as antimicrobial DNA gyrase inhibitors

Hamada H. H. Mohammed et al.

Summary: A series of N-4 piperazinyl ciprofloxacin derivatives were synthesized and showed broad antibacterial and antifungal activities. Some of the derivatives also exhibited inhibitory activity against DNA gyrase.

MOLECULAR DIVERSITY (2023)

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Article Chemistry, Medicinal

Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics

James Peek et al.

Summary: Bacterial resistance poses a threat to the effectiveness of current antibiotics. Hybrid antibiotics, composed of two covalently linked antibiotic entities, offer a strategy to overcome resistance. This study evaluates a series of semi-synthetic hybrid antibiotics formed by linking Kang A, a rifampicin analog, with fluoroquinolones. The results suggest that these hybrids may provide new avenues for generating antibiotics effective against drug-resistant infections.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

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Review Biochemistry & Molecular Biology

Emerging quinoline- and quinolone-based antibiotics in the light of epidemics

Paranjeet Kaur et al.

Summary: Pandemics are large-scale outbreaks of infectious diseases that pose a major threat to global health, and the development of antibiotics has played a significant role in treating these diseases effectively.

CHEMICAL BIOLOGY & DRUG DESIGN (2022)

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Article Chemistry, Medicinal

Design, Synthesis, in vitro and in silico Characterization of 2-Quinolone-L-alaninate-1,2,3-triazoles as Antimicrobial Agents

Oussama Moussaoui et al.

Summary: Due to the increasing antimicrobial resistance, there is an urgent need for the design and development of novel antimicrobial agents. In this study, we synthesized a series of compounds and investigated their antimicrobial and antifungal activities. The compounds exhibited significant antimicrobial activity and moderate antifungal activity.

CHEMMEDCHEM (2022)

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Review Chemistry, Medicinal

The Antibacterial Activity of Isatin Hybrids

Bi Liu et al.

Summary: Bacterial infections remain a major cause of patient morbidity and mortality worldwide, and their treatment is challenging due to rapidly evolving resistance mechanisms. Hybridization is a promising strategy for developing novel antibacterial drugs, and combining the pharmacophores of isatin with other antibacterial agents may create candidates with broad-spectrum activity against drug-resistant pathogens.

CURRENT TOPICS IN MEDICINAL CHEMISTRY (2022)

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Article Chemistry, Organic

Synthesis and biological evaluation of some novel hetroaryl quinolinone derivatives

Ghada E. Abd El-Ghani et al.

Summary: This study focused on synthesizing novel heterocyclic scaffolds with quinoline moiety and exploring their antimicrobial properties. The synthesized compounds showed promising antimicrobial and antifungal activities, with certain derivatives exhibiting superior efficacy compared to standard antibiotics and antifungals.

JOURNAL OF HETEROCYCLIC CHEMISTRY (2022)

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Review Chemistry, Organic

Medicinal perspective of quinazolinone derivatives: Recent developments and structure-activity relationship studies

Simranpreet K. Wahan et al.

Summary: Heterocyclic rings, especially quinazolinone derivatives, have attracted the interest of medicinal chemists for their potential pharmacological activities. These compounds have shown promising results in various fields, such as anticancer, anti-inflammatory, and antibacterial properties. Extensive literature and patent information on the synthetic schemes and biological activities of quinazolinone have been explored in this study.

JOURNAL OF HETEROCYCLIC CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

DFT based QSAR study on quinolone-triazole derivatives as antibacterial agents

Niloofar Ghasedi et al.

Summary: QSAR modeling was performed on 39 quinolone-triazole derivatives against gram-positive Staphylococcus aureus and gram-negative Pseudomonas aeruginosa bacteria. Molecular descriptors were extracted using quantum mechanical calculations, and hierarchical cluster analysis was used for subset division. The resulting models were internally and externally validated, highlighting specific descriptors that control antibacterial activity for each bacterium. New compounds with higher activities were proposed based on the models.

JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION (2022)

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Article Chemistry, Medicinal

Synthesis and potential antimicrobial activity of novel α-aminophosphonates derivatives bearing substituted quinoline or quinolone and thiazole moieties

Bilal Litim et al.

Summary: Novel alpha-aminophosphonates derivatives incorporating quinoline or quinolone, and coumarylthiazole or 5-phenylthiazol-2-amine moieties were synthesized and screened for antimicrobial activity. The compounds showed moderate to strong inhibitory activities against Gram-positive and Gram-negative bacteria, with some exhibiting excellent antifungal inhibition. Structure-activity relationship analysis indicated that certain structural moieties enhanced the inhibitory activity against microbial pathogens, suggesting the synthesized compounds as potential antimicrobial drug candidates.

MEDICINAL CHEMISTRY RESEARCH (2022)

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Article Biochemistry & Molecular Biology

Preliminary Studies of Antimicrobial Activity of New Synthesized Hybrids of 2-Thiohydantoin and 2-Quinolone Derivatives Activated with Blue Light

Agnieszka Kania et al.

Summary: Thiohydantoin and quinolone derivatives with broad-spectrum medical applications have been synthesized and analyzed for their antimicrobial properties. The effect of blue light irradiation on these compounds was also investigated. Preliminary results showed that some of the hybrid compounds exhibited bacteriostatic activity towards Gram-positive and Gram-negative bacteria, and this effect was enhanced by blue light activation.

MOLECULES (2022)

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Article Chemistry, Multidisciplinary

Ciprofloxacin-Tethered 1,2,3-Triazole Conjugates: New Quinolone Family Compounds to Upgrade Our Antiquated Approach against Bacterial Infections

Alka Agarwal et al.

Summary: A new series of ciprofloxacin conjugates containing 1,2,3-triazole were designed, synthesized, and evaluated for their antimicrobial activity. Some of the conjugates showed superior activity compared to the control drug ciprofloxacin, and exhibited low hemolysis on red blood cells.

ACS OMEGA (2022)

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Article Biochemistry & Molecular Biology

Recent insight into the biological activities and SAR of quinolone derivatives as multifunctional scaffold

Vishal Sharma et al.

Summary: This review introduces quinolone and its derivatives with different pharmacological properties, including antibacterial, anticancer, anti-HIV, antitubercular, and antimalarial activities. The focus is on the structural changes in the quinolone scaffold and its derivatives that lead to significant increase in therapeutic profile. Additionally, recent research findings on this scaffold are discussed.

BIOORGANIC & MEDICINAL CHEMISTRY (2022)

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Article Biochemistry & Molecular Biology

Novel heterocyclic 1,3,4-oxadiazole derivatives of fluoroquinolones as a potent antibacterial agent: Synthesis and computational molecular modeling

Tejeswara Rao Allaka et al.

Summary: Novel 1,3,4-oxadiazole compounds containing FQs derivatives were designed and synthesized, showing potent antibacterial activities against various bacteria and excellent antimycobacterial activity against drug-resistant M. smegmatis. Compounds FQs 6d and 6b demonstrated strong hydrogen bonding interactions with topoisomerase-IV from S. pneumoniae, contributing to their high antimicrobial efficacy.

MOLECULAR DIVERSITY (2022)

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Article Biochemistry & Molecular Biology

Thiazolidine-2,4-dione-linked ciprofloxacin derivatives with broad-spectrum antibacterial, MRSA and topoisomerase inhibitory activities

Hossameldin A. Aziz et al.

Summary: A series of ciprofloxacin/thiazolidine-2,4-dione hybrids were synthesized and some showed strong antibacterial activity against S. aureus, suggesting their potential as antibacterial agents. These compounds exert their effects by inhibiting DNA synthesis and exhibit promising activity against certain bacteria.

MOLECULAR DIVERSITY (2022)

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Article Chemistry, Medicinal

Synthesis, antibacterial evaluation and in silico study of DOTA-fluoroquinolone derivatives

Weitian Li et al.

Summary: A series of water-soluble fluoroquinolones based on DOTA modification were synthesized and characterized. These compounds exhibited potent antimicrobial activities against MRSA, P. aeruginosa, and E. coli. Among them, water-soluble quinolone 4c showed promising antibacterial potency with low cytotoxicity.

MEDICINAL CHEMISTRY RESEARCH (2022)

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Article Chemistry, Multidisciplinary

Synthesis and antibacterial activity of fluoroquinolones with sterically hindered phenolic moieties

S. V. Bukharov et al.

Summary: In this study, fluoroquinolone antibiotics modified with sterically hindered phenolic moieties were synthesized and evaluated for their antibacterial activity. The modification resulted in increased activity against certain strains of Staphylococcus aureus and St. epidermis, particularly when combined with a phosphonate moiety. Moxifloxacin with a 3,5-di-tert-butyl-4-hydroxybenzyl moiety exhibited higher activity against Escherichia coli compared to unmodified fluoroquinolones, while ciprofloxacin derivatives with sterically hindered phenolic moieties showed high activity against Gram-negative bacteria.

RUSSIAN CHEMICAL BULLETIN (2022)

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Article Chemistry, Medicinal

Design and synthesis of novel macrolones bridged with linkers from 11,12-positions of macrolides

Xie-Peng Liu et al.

Summary: The hybrids of macrolides and quinolones bridged with linkers from 11,12-cyclic carbamate of macrolides showed different structure-activity relationships and improved metabolic stability compared to telithromycin. The optimized macrolone was 38-fold more potent than telithromycin against A2058/2059-mutated Mycoplasma pneumoniae, potentially due to a novel mode of action between the carboxylic acid of quinolone moiety and the bacterial ribosome.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

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Article Biochemistry & Molecular Biology

Discovery of N-quinazolinone-4-hydroxy-2-quinolone-3-carboxamides as DNA gyrase B-targeted antibacterial agents

Wenjie Xue et al.

Summary: Emerging drug resistance highlights the need for new and effective antibiotics. This study used a 4-hydroxy-2-quinolone fragment to search for potential GyrB inhibitors and identified a novel and potent inhibitor, f1, with promising activity against drug-resistant bacteria. Further structural modification resulted in two more potent GyrB inhibitors, f4 and f14. Compound f1 exhibited superior antibacterial activity against MRSA, low toxicity to cells, and metabolic stability.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2022)

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Article

Study of Antimicrobial Effect of a New Fluoroquinolone Derivative Against Pathogenic Bacteria in Planktonic Form and Biofilm

Zeinab Taghavi et al.

Proceedings of the National Academy of Sciences, India. Section B (2022)

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Article Chemistry, Medicinal

N-Alkyl-2-Quinolonopyrones Demonstrate Antimicrobial Activity against ESKAPE Pathogens Including Staphylococcus aureus

Eoin Moynihan et al.

Summary: Antibiotic resistance has been increasing while the development of new antibiotics has been stagnant. This study introduces a novel suite of compounds that show significant antibiotic activity against several pathogens.

ACS MEDICINAL CHEMISTRY LETTERS (2022)

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Article Chemistry, Multidisciplinary

Quinolone-Rhodanine Hybrid Compounds: Synthesis and Biological Evaluation as Anti-Bacterial Agents

Yildiz Uygun Cebeci et al.

Summary: In this study, a series of new quinolone compounds were efficiently synthesized using 4-fluoroaniline and diethyl (ethoxymethylene)malonate as potential antimicrobial agents. The compounds showed significant antimicrobial activity, with compounds 9a and 9b demonstrating the highest activity.

CHEMISTRYSELECT (2022)

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Article Biochemistry & Molecular Biology

New potent ciprofloxacin-uracil conjugates as DNA gyrase and topoisomerase IV inhibitors against methicillin-resistant Staphylococcus aureus

Mohamed Samir et al.

Summary: A series of ciprofloxacin-uracil conjugates have been synthesized and evaluated for their antibacterial activities. The results showed that the new derivatives exhibited better activity against Gram-positive bacteria, with compounds 5b and 5g showing the highest activity and also demonstrating potent inhibitory activities against MRSA strains. Additionally, these compounds showed good inhibitory activities against DNA gyrase and topoisomerase IV.

BIOORGANIC & MEDICINAL CHEMISTRY (2022)

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Article Chemistry, Medicinal

Pyrimidine-conjugated fluoroquinolones as new potential broad-spectrum antibacterial agents

Yi-Min Tan et al.

Summary: Pyrimidine-conjugated fluoroquinolones demonstrated effective antibacterial activity against drug-resistant strains, with compound 1c exhibiting broad-spectrum antibacterial potency and low cytotoxicity. Compound 1c showed superior antibacterial activity against Enterococcus faecalis and exhibited lower trend for the development of drug-resistance compared to norfloxacin and ciprofloxacin. Further analysis revealed that compound 1c could induce ROS accumulation and interact with DNA, leading to bacterial death.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2022)

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Review Chemistry, Physical

A review: Structure-activity relationship and antibacterial activities of Quinoline based hybrids

Kajalben B. Patel et al.

Summary: This review summarizes quinoline-based hybrids with antibacterial activity and their structure-activity relationship (SAR), providing insights into the improvement of quinoline-based antibiotics, especially against multidrug-resistant bacterial strains.

JOURNAL OF MOLECULAR STRUCTURE (2022)

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Article Chemistry, Multidisciplinary

Synthesis and antibacterial activity evaluation of N (7) position-modified balofloxacins

Ge Hong et al.

Summary: A series of small-molecule fluoroquinolones were synthesized and screened for their antibacterial activity. Compound 2-e showed potent anti-MRSA activity, low toxicity towards normal cells, and the ability to disrupt MRSA cell membrane and wall. It also possessed good drug-like properties. These findings suggest that compound 2-e is highly promising for further investigation.

FRONTIERS IN CHEMISTRY (2022)

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Article Chemistry, Multidisciplinary

Synthesis, Antibacterial Evaluation and Molecular Docking Studies of 1,3,4-Oxadiazole-2(3H)-Thione-Norfloxacin Hybrids as Potent Antibacterial Agents

Jia-Bao Luo et al.

Summary: Novel 1,3,4-oxadiazole-2(3H)-thione-norfloxacin hybrids with potent antibacterial activity were designed and synthesized based on the pharmacophore hybridization concept. Among them, compound 3e showed the most promising antibacterial activity, exhibiting low toxicity and improved affinity towards DNA topoisomerase IV.

CHEMISTRYSELECT (2022)

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Review Pharmacology & Pharmacy

Fluoroquinolones Hybrid Molecules as Promising Antibacterial Agents in the Fight against Antibacterial Resistance

Ioana-Andreea Lungu et al.

Summary: The emergence of bacterial resistance has led to the search for new antibacterial agents, with fluoroquinolones being an important class of drugs due to their broad spectrum of activity. The design of fluoroquinolone hybrids with other antibacterial agents or active compounds has resulted in hybrids with superior antibacterial properties and additional biological effects.

PHARMACEUTICS (2022)

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Article Chemistry, Multidisciplinary

Synthesis of new 3-substituted quinolone derivatives with benzene sulfonamide group using hydrazine linker with their docking and antibacterial studies in vitro

Nishtha Saxena et al.

Summary: This study aimed to synthesize and test the antibacterial activity of a series of quinolone derivatives. The compounds showed bactericidal activity against various bacterial strains and displayed similar activity as Norfloxacin.

RESULTS IN CHEMISTRY (2022)

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Review Chemistry, Multidisciplinary

Design and synthesis of hybrid compounds as novel drugs and medicines

Abdulaziz H. Alkhzem et al.

Summary: The development of highly effective conjugate chemistry approaches is important for improving the quality of drugs and medicines. This paper reviews the design and application of hybrid compounds, highlighting their potential in areas such as anticancer therapies, non-viral gene therapy, antibiotic drug resistance prevention, and bacterial killing. The study also discusses the molecular precedents found in nature for designing hybrid compounds.

RSC ADVANCES (2022)

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Article Chemistry, Medicinal

Fluoroquinolone-3-carboxamide Amino Acid Conjugates: Synthesis, Antibacterial Properties And Molecular Modeling Studies

Riham M. Bokhtia et al.

Summary: This study aimed to synthesize and evaluate new fluoroquinolone-3-carboxamide amino acid conjugates as novel antibacterial agents, demonstrating strong selectivity against E. Coli. Additionally, the experimental results showed that the protecting groups on amino acids reduce antibacterial activity, but the synthesized conjugates are non-toxic to normal cell lines.

MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Synthesis and antimicrobial evaluation of new nitric oxide-donating fluoroquinolone/oxime hybrids

Hossameldin A. Aziz et al.

Summary: A new series of nitric oxide-donating fluoroquinolone/oximes were synthesized, showing higher activity in antitubercular and antibacterial evaluations. Mycobacterial DNA cleavage and molecular modeling were used to explain the bioactivity observed. Oximes3c-e were highly potent against Klebsiella pneumoniae, while ketone2c and oxime4c were more active against Staphylococcus aureus than ciprofloxacin.

ARCHIV DER PHARMAZIE (2021)

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Article Chemistry, Physical

Novel series of benzo[d]thiazolyl substituted-2-quinolone hybrids: Design, synthesis, biological evaluation and in-silico insights

Girish Bolakatti et al.

Summary: A novel series of benzo[d]thiazolyl substituted-2-quinolone hybrids were synthesized, showing significant cytotoxicity against cancer cells, especially compound 8f. Docking studies revealed important binding interactions of compounds 8f and 7f with EGFR tyrosine kinase. Additionally, compounds 7e, 7f, 8e, and 8f exhibited antibacterial activity, particularly against E. coli.

JOURNAL OF MOLECULAR STRUCTURE (2021)

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Article Chemistry, Medicinal

Potential antibacterial and antifungal activities of novel sulfamidophosphonate derivatives bearing the quinoline or quinolone moiety

Ismahene Bazine et al.

Summary: A series of new alpha-sulfamidophosphonate/sulfonamidophosphonate and cyclosulfamidophosphonate derivatives were designed and synthesized, showing potent inhibitory activities against both Gram-positive and -negative bacteria as well as excellent antifungal inhibition. The most active derivatives exhibited low minimum inhibitory concentrations and interesting zones of inhibition, highlighting the potential of these compounds for further applications.

ARCHIV DER PHARMAZIE (2021)

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Article Biochemistry & Molecular Biology

Antibiotic resistance and drug modification: Synthesis, characterization and bioactivity of newly modified potent ciprofloxacin derivatives

Abdulhakeem Alsughayer et al.

Summary: The main goal of this article is to develop new derivatives of commercial antibiotics and test their activities against different microorganisms. Various novel antibiotic derivatives were synthesized using different organic reagents and tested for their structural confirmation and bioactivities against gram-positive and gram-negative bacteria, showing high to moderate antibacterial activity. Additionally, these novel compounds demonstrated good effects against ciprofloxacin-resistant bacteria.

BIOORGANIC CHEMISTRY (2021)

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Article Biochemistry & Molecular Biology

Synthesis, molecular docking, and evaluation of antibacterial activity of 1,2,4-triazole-norfloxacin hybrids

Ping Yang et al.

Summary: A series of 1,2,4-triazole-norfloxacin hybrids were designed, synthesized, and evaluated for their in vitro antibacterial activity against common pathogens. The newly synthesized compounds showed superior antibacterial activity to norfloxacin, with high toxicity towards bacterial cells but good biocompatibility. Molecular docking analysis suggested strong affinity of the compounds for bacterial topoisomerase IV.

BIOORGANIC CHEMISTRY (2021)

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Review Infectious Diseases

Bacteriophages for ESKAPE: role in pathogenicity and measures of control

Amrita Patil et al.

Summary: The use of bacteriophages in combating antibiotic-resistant ESKAPE pathogens shows promise but also presents challenges, as bacteriophages can transfer genes that contribute to pathogen survival and resistance to antimicrobials. Extensive research on synthetic bacteriophages, bacteriophage cocktails, and their combination with antibiotics is needed to develop effective therapeutics against ESKAPE infections.

EXPERT REVIEW OF ANTI-INFECTIVE THERAPY (2021)

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Article Chemistry, Medicinal

The antibacterial activity of fluoroquinolone derivatives: An update (2018-2021)

Yanshu Jia et al.

Summary: Bacterial infection is a common disease and fluoroquinolones are widely used antibacterial agents. However, the emergence of drug resistance and more virulent pathogens highlights the need for developing new drugs. Research aims to summarize recent advances in fluoroquinolone derivatives and structure-activity relationships.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Pharmacology & Pharmacy

Synthesis, antitumor, antibacterial and urease inhibitory evaluation of new piperazinyl N-4 carbamoyl functionalized ciprofloxacin derivatives

Mohamed A. A. Abdel-Aal et al.

Summary: The study synthesized different derivatives of ciprofloxacin and evaluated their anticancer, antibacterial, and urease inhibitory activities. Some derivatives showed promising efficacy against breast and colon cancer cell lines, potentially serving as lead compounds for anticancer drug development, while others exhibited higher urease inhibitory activity than the parent drug.

PHARMACOLOGICAL REPORTS (2021)

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Article Pharmacology & Pharmacy

Hybrid Inhibitors of DNA Gyrase A and B: Design, Synthesis and Evaluation

Martina Durcik et al.

Summary: The discovery of multi-targeting ligands for bacterial enzymes is crucial in combating antimicrobial resistance. The designed hybrids effectively inhibit DNA gyrase and show antibacterial activity against Gram-negative pathogens, providing a promising therapeutic strategy.

PHARMACEUTICS (2021)

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Review Chemistry, Multidisciplinary

Prospects for Antibacterial Discovery and Development

Thomas M. Privalsky et al.

Summary: The increasing prevalence of multidrug-resistant bacteria has become an urgent health crisis, requiring renewed investment in the discovery and development of antibiotics. A multifaceted approach is necessary to address the antibacterial resistance crisis, with a focus on exploring validated antibacterial targets and lead molecules. Creative techniques, such as studying underexplored ecological niches or utilizing available data from genome mining efforts, can help in the search for new antibiotic leads.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

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Article Chemistry, Medicinal

Membrane active 7-thiazoxime quinolones as novel DNA binding agents to decrease the genes expression and exert potent anti-methicillin-resistant Staphylococcus aureus activity

Jin-Ping Chen et al.

Summary: A novel class of 7-thiazoxime quinolones has been developed as potential antimicrobial agents to combat quinolone resistance. Biological assays have shown that these compounds, particularly methyl acetate oxime derivative 6l, exhibit potent antibacterial activity against MRSA, with the ability to improve potency and alleviate bacterial resistance when used in combination with ciprofloxacin. The mechanism of action involves destroying the cell membrane, binding with DNA gyrase in MRSA DNA, and downregulating key genes, suggesting promise for combating MRSA infection.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Multidisciplinary

Design, Synthesis and Antibacterial Studies of 1,3,4-Oxadiazole-Fluoroquinolone Hybrids and Their Molecular Docking Studies

Ping Yang et al.

Summary: A series of novel hybrids based on fluoroquinolone skeleton were synthesized by introducing 1,3,4-oxadiazole derivatives to ciprofloxacin or norfloxacin at the C-7 site. In vitro antibacterial evaluation showed that some of the hybrids exhibited increased activity against Staphylococcus aureus and methicillin-resistant S. aureus, with some demonstrating bactericidal effects on standard bacteria. Molecular docking study revealed high binding affinity of certain hybrids to type IV topoisomerase.

CHEMISTRYSELECT (2021)

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Review Microbiology

Bacterial Antibiotic Resistance: The Most Critical Pathogens

Giuseppe Mancuso et al.

Summary: Overuse and misuse of antibiotics have accelerated the spread of antibiotic-resistant bacteria, leading to at least 700,000 deaths worldwide each year. Without new treatments, this number could rise to 10 million by 2050, posing a serious global health threat.

PATHOGENS (2021)

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Article Infectious Diseases

Mutational Diversity in the Quinolone Resistance-Determining Regions of Type-II Topoisomerases of Salmonella Serovars

Aqsa Shaheen et al.

Summary: Quinolone resistance in bacterial pathogens is primarily associated with mutations in specific regions of bacterial DNA enzymes. Research has been conducted on these mutations in Salmonella isolates globally, with efforts to understand the prevalence of these mutations in different serovars.

ANTIBIOTICS-BASEL (2021)

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Article Chemistry, Medicinal

Design, Synthesis, and Antibacterial Screening of Some Novel Heteroaryl-Based Ciprofloxacin Derivatives as DNA Gyrase and Topoisomerase IV Inhibitors

Lamya H. Al-Wahaibi et al.

Summary: A novel series of ciprofloxacin hybrids, including oxadiazole derivatives 2-6, showed good antibacterial activity against both Gram-positive and Gram-negative bacteria. However, they exhibited weak antifungal activity and compound 3 had the highest activity against Candida albicans.

PHARMACEUTICALS (2021)

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Review Chemistry, Medicinal

A key review on oxadiazole analogs as potential methicillin-resistant Staphylococcus aureus (MRSA) activity: Structure-activity relationship studies

Santosh Kumar Verma et al.

Summary: MRSA is becoming a major concern due to its rapid resistance development, prompting the need for novel antibiotics. The oxadiazole moiety serves as an interesting and adaptable molecular structure with potential for research and development as antibacterial agents. Studies on oxadiazole-containing derivatives as potent antibacterial agents against multidrug-resistant MRSA strains and exploring structure-activity relationships have been conducted, providing valuable insights for future drug development.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Chemistry, Medicinal

Current Landscape and Future Perspective of Oxazolidinone Scaffolds Containing Antibacterial Drugs

Qianqian Zhao et al.

Summary: The widespread use of antibiotics has led to a serious problem of bacterial resistance, making the study of new drug-resistant bacteria the main focus of antibacterial drug research. Oxazolidinone antibacterial drugs, such as linezolid and tedizolid, have good pharmacokinetic and pharmacodynamic characteristics, unique antibacterial mechanisms, and sensitivity to resistant bacteria.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

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Article Medicine, Research & Experimental

Conjugates of Ciprofloxacin and Amphiphilic Block Copoly(2-alkyl2-oxazolines)s Overcome Efflux Pumps and Are Active against CIP-Resistant Bacteria

Alina Romanovska et al.

Summary: Conjugation of antibiotics with amphiphilic polymers enhances their antibacterial activity by optimizing the hydrophobic/hydrophilic balance of the polymer tail, resulting in increased efficacy against pathogenic bacterial strains such as Staphylococcus aureus. The mechanism of action involves the amphiphilic polymer-conjugated antibiotics concentrating within bacterial cytoplasm, compensating for the loss of affinity to the target topoisomerase IV and leading to high antibacterial activity, while also slowing down resistance development in bacteria. Furthermore, these polymer-antibiotic conjugates show activity against antibiotic-resistant strains without being cytotoxic to human cells or causing lysis of blood cells.

MOLECULAR PHARMACEUTICS (2021)

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Article Chemistry, Multidisciplinary

Synthesis and Antimicrobial, Antiproliferative Evaluation of Novel Quinolone and Conazole Analogues via Conventional and Microwave Techniques

Sule Ceylan et al.

Summary: This study synthesized a series of 1,2,4-triazole derivatives through a series of synthetic steps and reactions. These compounds exhibited good antimicrobial and anticancer activities, with compound 14 a-e's Mannich base showing excellent activity against Mycobacterium smegmatis and compounds 8 a and 9 b having strong antiproliferative effects on HeLa cervical cancer cells.

CHEMISTRYSELECT (2021)

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Review Multidisciplinary Sciences

Antibacterial activity of medicinal plants against ESKAPE: An update

Priya Bhatia et al.

Summary: Antibiotic resistance poses a threat to global health, food security, and development, mainly due to misuse and overuse of antibiotics. ESKAPE pathogens are major causes of Hospital-Acquired Infections, leading to the urgent need for development of new antimicrobials. Plant-derived products are highlighted as potential treatments against ESKAPE pathogens due to their efficacy and minimal side effects.

HELIYON (2021)

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Review Biophysics

Sulfonamide drugs: structure, antibacterial property, toxicity, and biophysical interactions

Aben Ovung et al.

Summary: Sulfonamide drugs have various pharmacological activities and can be used to treat a variety of diseases, such as sulfamethazine for bacterial infections in veterinary medicine and sulfadiazine for treating toxoplasmosis in livestock.

BIOPHYSICAL REVIEWS (2021)

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Article Biochemistry & Molecular Biology

Design, synthesis, antimicrobial, and DNA gyrase inhibitory properties of fluoroquinolone-dichloroacetic acid hybrids

Israa A. Seliem et al.

CHEMICAL BIOLOGY & DRUG DESIGN (2020)

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Article Chemistry, Medicinal

Dual Escherichia coli DNA Gyrase A and B Inhibitors with Antibacterial Activity

Benedetta Fois et al.

CHEMMEDCHEM (2020)

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Article Chemistry, Medicinal

N-thiadiazole-4-hydroxy-2-quinolone-3-carboxamides bearing heteroaromatic rings as novel antibacterial agents: Design, synthesis, biological evaluation and target identification

Wenjie Xue et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Review Microbiology

Antimicrobial Resistance in ESKAPE Pathogens

David M. P. De Oliveira et al.

CLINICAL MICROBIOLOGY REVIEWS (2020)

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Article Microbiology

Global Evolution of Pathogenic Bacteria With Extensive Use of Fluoroquinolone Agents

Miklos Fuzi et al.

FRONTIERS IN MICROBIOLOGY (2020)

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Article Chemistry, Medicinal

Design, synthesis and structure-activity relationships of novel 15-membered macrolides: Quinolone/quinoline-containing sidechains tethered to the C-6 position of azithromycin acylides

Bing-Zhi Fan et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2020)

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Article Chemistry, Multidisciplinary

N1-Benzofused Modification of Fluoroquinolones Reduces Activity Against Gram-Negative Bacteria

Mark Laws et al.

ACS OMEGA (2020)

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Article Chemistry, Medicinal

A Semisynthetic Kanglemycin Shows In Vivo Efficacy against High-Burden Rifampicin Resistant Pathogens

James Peek et al.

ACS INFECTIOUS DISEASES (2020)

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Article Biochemistry & Molecular Biology

Conjugates of Ciprofloxacin and Levofloxacin with Cell-Penetrating Peptide Exhibit Antifungal Activity and Mammalian Cytotoxicity

Natalia Ptaszynska et al.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2020)

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Article Biochemistry & Molecular Biology

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