4.7 Article

A New Discovery of Unique 13-(Benzimidazolylmethyl)berberines as Promising Broad-Spectrum Antibacterial Agents

Related references

Note: Only part of the references are listed.
Article Chemistry, Medicinal

An unanticipated discovery towards novel naphthalimide corbelled aminothiazoximes as potential anti-MRSA agents and allosteric modulators for PBP2a

Peng-Li Zhang et al.

Summary: The study introduced a novel antibacterial framework and demonstrated through experiments that the new compound exhibited strong inhibition against MRSA, showed excellent membrane selectivity, and effectively alleviated bacterial resistance.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

Natural Berberine-derived Azolyl Ethanols as New Structural Antibacterial Agents against Drug-Resistant Escherichia coli

Hang Sun et al.

Summary: Natural berberine-derived azolyl ethanols were designed and synthesized as new structural antibacterial agents to combat bacterial resistance, with potent activity against multidrug-resistant Escherichia coli. These compounds could rapidly kill bacteria and eradicate biofilms, aiding in alleviating bacterial resistance development.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

Novel metronidazole-derived three-component hybrids as promising broad-spectrum agents to combat oppressive bacterial resistance

Fen-Fen Li et al.

Summary: This study developed a class of novel metronidazole-derived three-component hybrids as promising antibacterial therapeutic alternatives. The active molecule 6b showed excellent ability to suppress the growth of drug-resistant E. coli and could effectively retard the development of bacterial drug resistance. Mechanism exploration revealed that 6b could destruct the bacterial cytoplasmic membrane, obstruct DNA replication, and cause metabolic stagnation and the accumulation of reactive oxygen species.

BIOORGANIC CHEMISTRY (2022)

Review Chemistry, Inorganic & Nuclear

Tailoring supramolecular short peptide nanomaterials for antibacterial applications

Manzar Abbas et al.

Summary: The rise of bacterial resistance to antibiotics highlights the need for new-generation nanomaterials with antibacterial properties and biosafety. Short-peptide based supramolecular nanomaterials show great potential as antibacterial agents due to their ease of fabrication, favorable physicochemical properties, and diverse functionalities. This article provides an overview of the design and therapeutic modes of action of short peptides, as well as the biosafety and antibacterial mechanisms of supramolecular short peptide composites and biomineralized nanomaterials.

COORDINATION CHEMISTRY REVIEWS (2022)

Article Chemistry, Medicinal

Dihydropyrimidinone imidazoles as unique structural antibacterial agents for drug-resistant gram-negative pathogens

Xi Yang et al.

Summary: The health crisis caused by severe multidrug resistance is driving the need for new alternative antibacterial drugs. A library of structurally unique dihydropyrimidinone imidazoles was developed as potential antibacterial agents. One compound, sulfamethoxazole hybridized dihydropyrimidinone imidazole 8b, exhibited excellent antibacterial activity against multidrug-resistant K. pneumonia and A. baumanii, and showed low cytotoxicity and good biofilm inhibition ability.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

Discovery of unique thiazolidinone-conjugated coumarins as novel broad spectrum antibacterial agents

Xun-Cai Yang et al.

Summary: Unique coumarin conjugates with thiazolidinone were utilized as antibacterial modulators to combat multidrug-resistant bacterial infections. The indole-incorporated coumarin thiazolidinone conjugate 14a exhibited broad-spectrum antibacterial activity, low cytotoxicity, and favorable pharmacokinetic properties.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

Unique Carbazole-Oxadiazole Derivatives as New Potential Antibiotics for Combating Gram-Positive and -Negative Bacteria

Yun-Peng Xie et al.

Summary: Novel carbazole-oxadiazoles were developed as potential antibacterial agents and showed predominant inhibitory effects on both Gram-positive and -negative bacteria, especially in impeding the growth of MRSA and Pseudomonas aeruginosa ATCC 27853. The compounds exhibited low cytotoxicity and low tendency to develop resistance, and could disintegrate bacterial cell membranes to exert excellent antibacterial effects.

JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

Coumarin thiazoles as unique structural skeleton of potential antimicrobial agents

Xun-Cai Yang et al.

Summary: A novel type of coumarin thiazoles were synthesized and exhibited favorable inhibitory potency against various strains, especially methicillin-resistant Staphylococcus aureus (MRSA). The active compound showed low toxicity towards mammalian cells, effectively eradicated MRSA biofilms, and had a low probability of engendering drug resistance.

BIOORGANIC CHEMISTRY (2022)

Article Biochemistry & Molecular Biology

Aloe emodin-conjugated sulfonyl hydrazones as novel type of antibacterial modulators against S. aureus 25923 through multifaceted synergistic effects

Zhao Deng et al.

Summary: Aloe emodin-conjugated sulfonyl hydrazones, specifically AEBH-5a, show high selectivity and antibacterial activity against S. aureus, being able to eliminate biofilms and reduce antibiotic resistance. The mechanisms of action include disruption of bacterial membrane integrity, induction of oxidative stress, inhibition of lactate dehydrogenase activity, and metabolic inactivation. In silico studies also suggest favorable bioavailability and drug-likeness profiles for AEBH-5a.

BIOORGANIC CHEMISTRY (2022)

Article Chemistry, Medicinal

Discovery of novel phenylhydrazone-based oxindole-thiolazoles as potent antibacterial agents toward Pseudomonas aeruginosa

Fen-Fen Li et al.

Summary: This study developed a series of phenylhydrazone-based oxindole-thiolazole compounds, among which compound 4e exhibited potent antibacterial activity and could effectively inhibit bacterial growth and resistance. Mechanism studies revealed that compound 4e could disrupt bacterial cytoplasmic membrane, cause leakage of cellular contents, induce metabolic stagnation and intracellular oxidative stress, and interact with DNA.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Medicinal

An unanticipated discovery of novel naphthalimidopropanediols as potential broad-spectrum antibacterial members

Peng-Li Zhang et al.

Summary: Constructing a new antibacterial framework is an effective strategy against drug resistance. This study discovered a novel class of potential broad-spectrum antibacterial agents, called NIOLs. These active compounds showed high selectivity towards bacterial membranes and could effectively inhibit bacterial growth by disrupting the membranes, interfering with the antioxidant defense systems, and eradicating strains within biofilms. Furthermore, they exhibited low cytotoxicity. These findings provide a hopeful solution for combating drug resistance.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2022)

Article Chemistry, Multidisciplinary

Synthesis and Biological Evaluation of Quinazolonethiazoles as New Potential Conquerors towards Pseudomonas Aeruginosa

Jie Wang et al.

Summary: Novel quinazolonthiazoles, particularly compound 7d, exhibited superior antimicrobial activity with low toxicity, suggesting potential mechanisms of action involving disruption of bacterial membrane permeability and interference with DNA-topoisomerase IV interactions. These findings provide valuable insights for the development of quinazolonthiazoles as new antimicrobial agents against drug-resistant pathogens.

CHINESE JOURNAL OF CHEMISTRY (2021)

Article Chemistry, Medicinal

Plant isoquinoline alkaloids: Advances in the chemistry and biology of berberine

Sneha Singh et al.

Summary: Isoquinoline alkaloids are important plant bioactives with diverse structures and various biological activities, including anticancer, antidiabetic, anti-inflammatory, and antimicrobial effects. Berberine, as one of the most prominent bioactive compounds in this class, possesses broad-spectrum pharmacological activities and is widely researched.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Biochemistry & Molecular Biology

A comprehensive review on the biological interest of quinoline and its derivatives

Basavarajaiah Suliphuldevara Matada et al.

Summary: Quinoline and its derivatives are important compounds with diverse biological activities, making them significant for drug development. Many scientific communities have conducted research on these compounds and evaluated their biological activities and medicinal value.

BIOORGANIC & MEDICINAL CHEMISTRY (2021)

Article Chemistry, Multidisciplinary

Solution Structure of Ternary Complex of Berberine Bound to a dGMP-Fill-In Vacancy G-Quadruplex Formed in the PDGFR-β Promoter

Kai-Bo Wang et al.

Summary: The high-resolution NMR structure of a ternary complex of berberine bound to the dGMP-fill-in PDGFR-beta vG4 in potassium solution reveals the first small-molecule complex structure of a fill-in vG4. This complex provides insights into the binding mechanism and rational design of berberine analogues targeting PDGFR-beta vG4.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2021)

Article Food Science & Technology

Anti-biofilm activity of N-Mannich bases of berberine linking piperazine against Listeria monocytogenes

Joo-Won Kim et al.

Summary: The study demonstrated that N-Mannich bases of berberine linking piperazine (MBP), specifically MBP5 and MBP6, have significant anti-biofilm activity against Listeria monocytogenes. These compounds effectively reduced biofilm formation and viability of the bacteria on various surfaces, suggesting their potential use as promising anti-biofilm agents.

FOOD CONTROL (2021)

Review Chemistry, Medicinal

Pipeline of anti-Mycobacterium abscessus small molecules: Repurposable drugs and promising novel chemical entities

Anna Egorova et al.

Summary: This review discusses recent advances in novel small-molecule agents for M. abscessus, focusing on the activity, mode of action, and structure-activity relationship of promising inhibitors from different chemical classes. Additionally, it summarizes other interesting small molecules in early drug development stages and current knowledge about the efficacy of repurposable drugs.

MEDICINAL RESEARCH REVIEWS (2021)

Review Biochemistry & Molecular Biology

An insight into the medicinal attributes of berberine derivatives: A review

Sobhi Gaba et al.

Summary: Berberine, a plant-derived isoquinoline alkaloid, has shown remarkable therapeutic diversity and potential for the discovery of new therapeutic agents. Despite its clinical utility being compromised by undesirable pharmacokinetic properties, structural modifications have been made to improve its therapeutic efficacy, leading to significant advancements in its medicinal chemistry. This review provides a comprehensive overview of recent advancements in the field and serves as a valuable guide for the rational design of berberine-based compounds.

BIOORGANIC & MEDICINAL CHEMISTRY (2021)

Article Chemistry, Multidisciplinary

Design and Synthesis of Sulfanilamide Aminophosphonates as Novel Antibacterial Agents towards Escherichia coli

Juan Wang et al.

Summary: A new class of sulfanilamide aminophosphonates showed activity against drug resistant bacteria and low toxicity to human cells, indicating potential as novel antibacterial agents. Mechanistic studies revealed that the compound disrupted bacterial cell membrane and formed a stable complex leading to bacterial death.

CHINESE JOURNAL OF CHEMISTRY (2021)

Article Chemistry, Medicinal

Identification of Unique Quinazolone Thiazoles as Novel Structural Scaffolds for Potential Gram-Negative Bacterial Conquerors

Jie Wang et al.

Summary: A class of quinazolone thiazoles has been identified as potential antibacterial conquerors with favorable bacteriostatic efficiencies. Compound 5j, featuring the 4-trifluoromethylphenyl group, showed superior performance against Escherichia coli and Pseudomonas aeruginosa, and could hinder the formation of bacterial biofilms by triggering reactive oxygen species generation. Additionally, compound 5j exhibited powerful antibacterial properties by disintegrating bacterial membranes, suppressing dehydrogenase, and intercalating into DNA.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Medicinal

Design, Synthesis, and Biological Evaluation of Membrane-Active Bakuchiol Derivatives as Effective Broad-Spectrum Antibacterial Agents

Hongxia Li et al.

Summary: This study designed and synthesized a series of new membrane-active bakuchiol derivatives, with compound 28 showing potent antibacterial activity against various bacteria and strong in vivo antibacterial efficacy in murine corneal infection models. This design strategy is expected to provide an effective solution to the antibiotic crisis.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Review Chemistry, Medicinal

An Overview of the Biological Activity of Pyrrolo[3,4-c]pyridine Derivatives

Anna Wojcicka et al.

Summary: Pyrrolo[3,4-c]pyridine derivatives have broad pharmacological properties, mainly used in analgesic, sedative, and treatment of diseases related to the nervous and immune systems. They also show activities against diabetes, mycobacterial infections, viruses, and tumors.

PHARMACEUTICALS (2021)

Article Biochemistry & Molecular Biology

Molecular design and preparation of 2-aminothiazole sulfanilamide oximes as membrane active antibacterial agents for drug resistant Acinetobacter baumannii

Juan Wang et al.

Summary: A series of new membrane active antibacterial agents were developed with good biocompatibility and ability to eradicate biofilm. Compound 10c showed superiority in treating drug-resistant A. baumannii infection and effectively interfered with cellular oxidoreduction balance by disturbing the cell membrane.

BIOORGANIC CHEMISTRY (2021)

Article Chemistry, Applied

Antimicrobial mechanism of alkyl gallates against Escherichia coli and Staphylococcus aureus and its combined effect with electrospun nanofibers on Chinese Taihu icefish preservation

Yu-gang Shi et al.

Summary: This study found that the length of alkyl gallates plays a crucial role in their antibacterial activity, with octyl gallate exhibiting excellent bactericidal activity through a multiple bactericidal mechanism and unique advantages in maintaining food freshness.

FOOD CHEMISTRY (2021)

Article Agriculture, Multidisciplinary

Natural Berberine-Hybridized Benzimidazoles as Novel Unique Bactericides against Staphylococcus aureus

Hang Sun et al.

Summary: Berberine-hybridized benzimidazoles, such as the 2,4-dichlorobenzyl derivative 7d, showed potent antibacterial efficacy against Staphylococcus aureus, with the ability to eradicate bacterial biofilm and low toxicity towards mammalian cells. Combination with norfloxacin enhanced the antibacterial efficacy, while development of bacterial resistance was not observed. Mechanism studies indicated that the active molecule 7d damaged membrane integrity, stimulated ROS generation, and bound with DNA and S. aureus sortase A, exerting powerful antibacterial ability in treating S. aureus in the livestock industry.

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY (2021)

Article Biochemistry & Molecular Biology

Novel carbazole-oxadiazoles as potential Staphylococcus aureus germicides

Yun-Peng Xie et al.

Summary: A newly synthesized antibacterial compound showed effective inhibitory activity against Staphylococcus aureus and other bacteria, with low tendency to induce resistance. The compound also demonstrated abilities to disrupt bacterial biofilm and interfere with DNA, while exhibiting low toxicity towards human cells.

PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY (2021)

Editorial Material Multidisciplinary Sciences

MICROBIOLOGY Giving antibiotics an assist

Thien-Fah Mah

SCIENCE (2021)

Article Multidisciplinary Sciences

Inhibitors of bacterial H2S biogenesis targeting antibiotic resistance and tolerance

Konstantin Shatalin et al.

Summary: The emergence of resistance to clinical antibiotics has prompted the development of a new antimicrobial strategy targeting the bacterial hydrogen sulfide (H2S) defense system. Inhibitors of the bacterial cystathionine g-lyase (CSE) have been found to enhance the effectiveness of bactericidal antibiotics against major human pathogens such as Staphylococcus aureus and Pseudomonas aeruginosa. These inhibitors also disrupt bacterial tolerance, reduce biofilm formation, and decrease the number of persister bacteria surviving antibiotic treatment.

SCIENCE (2021)

Article Chemistry, Medicinal

Development of Amphiphilic Coumarin Derivatives as Membrane-Active Antimicrobial Agents with Potent In Vivo Efficacy against Gram-Positive Pathogenic Bacteria

Rongcui Zhong et al.

Summary: Compound 25, a newly designed amphiphilic coumarin derivative, showed potent antibacterial activity against Gram-positive bacteria, including MRSA, with low hemolytic activity and toxicity. It can quickly kill bacteria by disrupting cell membranes and demonstrated excellent efficacy in a murine corneal infection caused by Staphylococcus aureus. This suggests that compound 25 has great potential as a potent antimicrobial agent for treating drug-resistant Gram-positive bacterial infections.

ACS INFECTIOUS DISEASES (2021)

Article Biochemistry & Molecular Biology

Aloe-emodin derived azoles as a new structural type of potential antibacterial agents: design, synthesis, and evaluation of the action on membrane, DNA, and MRSA DNA isomerase

Xin-Yuan Liang et al.

Summary: Novel aloe-emodin azoles were developed as potential antibacterial agents, with tetrazolyl aloe-emodin 4b showing effective activity against MRSA, low cytotoxicity against human cells, and a possible mechanism of disrupting MRSA membrane integrity and forming a supramolecular complex with DNA.

RSC MEDICINAL CHEMISTRY (2021)

Review Chemistry, Multidisciplinary

Ethnobotany and the Role of Plant Natural Products in Antibiotic Drug Discovery

Gina Porras et al.

Summary: The crisis of antibiotic resistance highlights the importance of exploring plant natural products as a potential source of antibacterial compounds. This review systematically examines the antibacterial activity of 459 plant-derived compounds, with a focus on 183 compounds that show promising potential as antibiotics. The rich chemodiversity and clinical effectiveness of plant NPs make them a valuable resource for future antibiotic discovery and development efforts.

CHEMICAL REVIEWS (2021)

Review Biochemistry & Molecular Biology

The Science of Antibiotic Discovery

Kim Lewis

Article Chemistry, Medicinal

Development of Bis-cyclic Imidazolidine-4-one Derivatives as Potent Antibacterial Agents

Minghui Wang et al.

JOURNAL OF MEDICINAL CHEMISTRY (2020)

Article Multidisciplinary Sciences

A selective membrane-targeting repurposed antibiotic with activity against persistent methicillin-resistant Staphylococcus aureus

Wooseong Kim et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2019)

Article Chemistry, Medicinal

Synthesis and bioactivities study of new antibacterial peptide mimics: The dialkyl cationic amphiphiles

En Zhang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

The synthesis and antistaphylococcal activity of 9, 13-disubstituted berberine derivatives

Jing Wang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2017)

Article Chemistry, Organic

Metal-Free TEMPO-Promoted C(sp3)-H Amination To Afford Multisubstituted Benzimidazoles

Ding Xue et al.

JOURNAL OF ORGANIC CHEMISTRY (2014)

Review Chemistry, Medicinal

Comprehensive Review in Current Developments of Imidazole-Based Medicinal Chemistry

Ling Zhang et al.

MEDICINAL RESEARCH REVIEWS (2014)