4.6 Review

Benzimidazole-Triazole Hybrids as Antimicrobial and Antiviral Agents: A Systematic Review

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NATURE MICROBIOLOGY (2021)

Article Chemistry, Physical

New 1,2,3-triazole containing benzimidazolone derivatives: Syntheses, crystal structures, spectroscopic characterizations, Hirshfeld surface analyses, DFT calculations, anti-corrosion property anticipation, and antibacterial activities

Asmaa Saber et al.

Summary: A new series of triazole derivatives containing a benzimidazolone moiety were synthesized using 1,3-dipolar cycloaddition and click chemistry, with their structures characterized and confirmed by spectroscopy and X-ray crystallography. The compounds showed promising anti-corrosion properties for iron and exhibited antibacterial activities against various microbial strains.

JOURNAL OF MOLECULAR STRUCTURE (2021)

Article Biochemistry & Molecular Biology

Synthesis, Identification, Computer-Aided Docking Studies, and ADMET Prediction of Novel Benzimidazo-1,2,3-triazole Based Molecules as Potential Antimicrobial Agents

Huda R. M. Rashdan et al.

Summary: The study describes a synthetic method for producing new compounds with promising antimicrobial activity against bacterial strains. Through molecular docking studies and in vitro experiments, the synthesized compounds were found to exhibit significant potential as antimicrobial agents.

MOLECULES (2021)

Article Biochemistry & Molecular Biology

Synthesis and Pharmacological Evaluation of Novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole Derivatives as Promising Anxiolytic and Analgesic Agents

Dmitriy V. V. Maltsev et al.

Summary: A series of novel compounds were synthesized through alkylation, with compounds 2d and 3b showing significant analgesic and anxiolytic potentials in various biological activity tests. In silico analysis indicated that the high anxiolytic activity of compound 3b may be attributed to its interaction with specific receptors.

MOLECULES (2021)

Article Chemistry, Medicinal

Furazans in Medicinal Chemistry

Ross S. Mancini et al.

Summary: The article provides a summary of the application of furazan-containing molecules in medicinal chemistry and drug development, with a focus on projects that have reached clinical or preclinical stages of development.

JOURNAL OF MEDICINAL CHEMISTRY (2021)

Article Chemistry, Multidisciplinary

Synthesis, molecular docking, antibacterial, and anti-inflammatory activities of benzimidazole-containing tricyclic systems

Vinuta Kamat et al.

Summary: This study reported the synthesis of benzimidazole-containing tricyclic systems with significant antimicrobial and anti-inflammatory activities, with compound 5b showing excellent efficacy. The hydroxyl group on the aromatic ring plays an important role in biological activity, and the synthesized compounds displayed promising minimum inhibitory concentration values against tested strains. The molecular docking study showed good binding interactions against Escherichia coli, supporting the in vitro findings.

JOURNAL OF THE CHINESE CHEMICAL SOCIETY (2021)

Article Chemistry, Multidisciplinary

Antibacterial and antiviral activities and action mechanism of flavonoid derivatives with a benzimidazole moiety

Mei Chen et al.

Summary: In this study, a class of novel benzimidazole-containing flavonoid derivatives were synthesized and exhibited promising antibacterial and antiviral activities. Compound 4e showed outstanding antibacterial activity against Rs, while compound 4n displayed remarkable curative, protective, and inactivating activities against TMV. These findings suggest that benzimidazole-containing flavonoid derivatives have potential as agricultural antibacterial and antiviral agents.

JOURNAL OF SAUDI CHEMICAL SOCIETY (2021)

Review Chemistry, Medicinal

1,2,4-Triazoles as Important Antibacterial Agents

Malgorzata Strzelecka et al.

Summary: Compounds containing the 1,2,4-triazole ring exhibit multidirectional biological activity and significant antibacterial properties, making them promising candidates for the development of novel antimicrobial agents to combat microbial resistance issues. Further research and rational design are needed to fully harness the potential of this scaffold.

PHARMACEUTICALS (2021)

Review Pharmacology & Pharmacy

A Comprehensive Account on Recent Progress in Pharmacological Activities of Benzimidazole Derivatives

Shejuti Rahman Brishty et al.

Summary: Benzimidazole derivatives, as a class of potential drugs, play an important role in the field of medicine with broad biological activity and structure-activity relationships. These compounds show a wide range of pharmacological properties from antibacterial effects to the world's most deadly diseases.

FRONTIERS IN PHARMACOLOGY (2021)

Review Chemistry, Multidisciplinary

Green synthesis of biologically active heterocycles of medicinal importance: a review

R. Nishanth Rao et al.

Summary: Heterocyclic moieties are essential for 80% of commercial medicines, yet many synthetic methods are not sustainable, prompting the need for eco-friendly strategies like microwave-assisted synthesis and nanoparticle-catalysed synthesis. Other sustainable methods include solvent-free synthesis, ionic liquid-supported synthesis, organic synthesis in water, sonochemical synthesis, and combinatorial synthesis.

ENVIRONMENTAL CHEMISTRY LETTERS (2021)

Review Chemistry, Multidisciplinary

A review on 'triazoles': their chemistry, synthesis and pharmacological potentials

Deepali Dixit et al.

Summary: Triazole compounds are cyclic compounds with at least two different elements in the ring, showing versatile biological activities and being widely used in various drug classes.

JOURNAL OF THE IRANIAN CHEMICAL SOCIETY (2021)

Article Pharmacology & Pharmacy

Antihypertensive Effect of a Novel Angiotensin II Receptor Blocker Fluorophenyl Benzimidazole: Contribution of cGMP, Voltage-dependent Calcium Channels, and BKCa Channels to Vasorelaxant Mechanisms

Hina Iqbal et al.

Summary: The study introduces a novel angiotensin II receptor blocker FPD as an antihypertensive agent in the SHR model of hypertension. FPD effectively decreased blood pressure in SHR, relaxed superior mesenteric arteries, and inhibited angiotensin II-induced contraction by increasing tissue cGMP levels, inhibiting L-type calcium channels, and opening BKCa channels. Moreover, FPD showed good safety in toxicity evaluation and demonstrated potential as a vasorelaxant with cGMP, L-type calcium channels, and BKCa channels as putative targets.

FRONTIERS IN PHARMACOLOGY (2021)

Article Biochemistry & Molecular Biology

New quinoline-triazole conjugates: Synthesis, and antiviral properties against SARS-CoV-2

Israa A. Seliem et al.

Summary: Novel small molecules with quinoline scaffolds were synthesized and assessed for their anti-SARS-CoV2 activity, with compounds 10g and 12c showing high potency and significant efficacy in comparison to reference drugs.

BIOORGANIC CHEMISTRY (2021)

Review Chemistry, Physical

Recent Progress in Catalytic Synthesis of 1,2,3-Triazoles

Antonio De Nino et al.

Summary: This review summarizes the progress achieved in the synthesis of 1,2,3-triazoles from 2015 to today, focusing particularly on the development of new catalytic and eco-compatible approaches. The report is subdivided based on the degree of functionalization of the molecules, with emphasis on the role of the catalyst employed for each specific approach.

CATALYSTS (2021)

Review Infectious Diseases

Synthesis of Antimicrobial Benzimidazole-Pyrazole Compounds and Their Biological Activities

Maria Marinescu

Summary: The synthesis of new compounds with antimicrobial and antiviral properties is crucial in combating the COVID-19 pandemic. Benzimidazole and pyrazole compounds possess diverse biological activities, making them important in medicinal chemistry.

ANTIBIOTICS-BASEL (2021)

Article Chemistry, Multidisciplinary

New 1H-benzimidazole-2-yl hydrazones with combined antiparasitic and antioxidant activity

Maria A. Argirova et al.

Summary: A series of new compounds combining anthelmintic with antioxidant properties were synthesized and found to be more active than clinically used anthelmintic drugs in vitro. Two of these compounds showed the best radical scavenging ability and their antioxidant mechanisms were elucidated through DFT calculations. It was demonstrated that these compounds are capable of reacting with various free radicals.

RSC ADVANCES (2021)

Article Medicine, General & Internal

Potential antidiabetic activity of benzimidazole derivative albendazole and lansoprazole drugs in different doses in experimental type 2 diabetic rats

Burak Dik et al.

Summary: The study revealed that albendazole and lansoprazole treatments could potentially act as drugs or in combination with antidiabetic drugs in type 2 diabetic (T2D) treatment through multiple antidiabetic mechanisms, such as AMPK and PPAR. Developing more specific substances with benzimidazole scaffold may help in creating a more effective treatment strategy.

TURKISH JOURNAL OF MEDICAL SCIENCES (2021)

Review Pharmacology & Pharmacy

Triazole analogues as potential pharmacological agents: a brief review

Sachin Kumar et al.

Summary: This review focuses on the recent synthetic procedures of the triazole moiety, which exhibit various pharmacological activities such as antimicrobial, anticonvulsant, anti-inflammatory, analgesic, antitubercular, anthelmintic, antioxidant, antimalarial, antiviral, etc. The review highlights the current status of triazole compounds with different multitarget pharmacological activities, emphasizing their wide usage in various potential activities.

FUTURE JOURNAL OF PHARMACEUTICAL SCIENCES (2021)

Article Biochemistry & Molecular Biology

Benzimidazole-1,2,3-triazole hybrid molecules: synthesis and study of their interaction with G-quadruplex DNA

Padma S. Singu et al.

Summary: A series of new benzimidazole-1,2,3-triazole hybrid derivatives were synthesized via 'click' reaction, with compound 4f showing high selectivity for G-quadruplex DNA and inducing G2/M phase arrest and apoptosis. Experimental results suggest that compound 4f may be a G-quadruplex DNA groove binding molecule with potential anticancer activity.

RSC MEDICINAL CHEMISTRY (2021)

Article Biochemistry & Molecular Biology

Synthesis and biological evaluation of new benzimidazole-1,2,3-triazole hybrids as potential α-glucosidase inhibitors

Nafise Asemanipoor et al.

BIOORGANIC CHEMISTRY (2020)

Article Chemistry, Physical

A step-by-step synthesis of triazole-benzimidazole-chalcone hybrids: Anticancer activity in human cells+

Amar Djemoui et al.

JOURNAL OF MOLECULAR STRUCTURE (2020)

Article Chemistry, Medicinal

Synthesis and antidiabetic evaluation of benzimidazole-tethered 1,2,3-triazoles

Laxmi Deswal et al.

ARCHIV DER PHARMAZIE (2020)

Article Biochemistry & Molecular Biology

Synthesis and neuroprotective effects of novel chalcone-triazole hybrids

Pichjira Sooknual et al.

BIOORGANIC CHEMISTRY (2020)

Article Chemistry, Multidisciplinary

Structure based approach for twin-enzyme targeted benzimidazolyl-1,2,4-triazole molecular hybrids as antifungal agents

Radha Ahuja et al.

ARABIAN JOURNAL OF CHEMISTRY (2020)

Article Chemistry, Multidisciplinary

Synthesis and Antimicrobial Activity of Novel Bis-1,2,3-triazol-1H-4-yl-substituted Aryl Benzimidazole-2-thiol Derivatives

Y. Aparna et al.

RUSSIAN JOURNAL OF GENERAL CHEMISTRY (2020)

Review Chemistry, Multidisciplinary

Synthesis of anti-allergic drugs

Shiyang Zhou et al.

RSC ADVANCES (2020)

Article Chemistry, Multidisciplinary

Design, synthesis and antifungal evaluation of novel benzimidazole tertiary amine type of fluconazole analogues

Rani S. Kankate et al.

ARABIAN JOURNAL OF CHEMISTRY (2019)

Review Chemistry, Medicinal

Triazole derivatives and their antiplasmodial and antimalarial activities

Xue-Mei Chu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

Synthesis and AChE-Inhibitory Activity of New Benzimidazole Derivatives

Ulviye Acar Cevik et al.

MOLECULES (2019)

Review Chemistry, Medicinal

Comprehensive review on the anti-bacterial activity of 1,2,3-triazole hybrids

Bo Zhang

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Review Chemistry, Medicinal

Antimicrobial Potential of Benzimidazole Derived Molecules

Yogita Bansal et al.

MINI-REVIEWS IN MEDICINAL CHEMISTRY (2019)

Article Chemistry, Medicinal

Design, synthesis and docking studies of benzimidazole derivatives as potential EGFR inhibitors

Ismail Celik et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Review Chemistry, Medicinal

Recent Advances in Antiviral Benzimidazole Derivatives: A Mini Review

Afshan Kanwal et al.

PHARMACEUTICAL CHEMISTRY JOURNAL (2019)

Review Biochemistry & Molecular Biology

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Khurshed Bozorov et al.

BIOORGANIC & MEDICINAL CHEMISTRY (2019)

Article Multidisciplinary Sciences

Strategies Towards the Synthesis of N2-Substituted 1,2,3-Triazoles

Rodrigo Octavio M. A. De Souza et al.

ANAIS DA ACADEMIA BRASILEIRA DE CIENCIAS (2019)

Article Chemistry, Medicinal

New Application of Neomycin B-Bisbenzimidazole Hybrids as Antifungal Agents

Nishad Thamban Chandrika et al.

ACS INFECTIOUS DISEASES (2018)

Article Biochemistry & Molecular Biology

Synthesis, anti-bacterial and anti-protozoal activities of amidinobenzimidazole derivatives and their interactions with DNA and RNA

Andrea Bistrovic et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Design, Synthesis and Anticancer Screening of Novel Benzothiazole-Piperazine-1,2,3-Triazole Hybrids

Mohamed R. Aouad et al.

MOLECULES (2018)

Article Chemistry, Medicinal

Novel 2-Arylbenzimidazole derivatives as multi-targeting agents to treat Alzheimer's disease

Oya Unsal-Tan et al.

MEDICINAL CHEMISTRY RESEARCH (2017)

Article Chemistry, Organic

Green Microwave Synthesis and Antimicrobial Evaluation of Novel Triazoles

Nadjet Rezki

ORGANIC PREPARATIONS AND PROCEDURES INTERNATIONAL (2017)

Article Chemistry, Medicinal

PREDICTION AND STUDY OF ANTICONVULSANT PROPERTIES OF BENZIMIDAZOLE DERIVATIVES

P. M. Vasil'ev et al.

PHARMACEUTICAL CHEMISTRY JOURNAL (2017)

Article Chemistry, Organic

Synthesis of new 1,2,3-triazole linked benzimidazole molecules as anti-proliferative agents

Ishani I. Sahay et al.

SYNTHETIC COMMUNICATIONS (2017)

Article Biochemistry & Molecular Biology

Synthesis, in vitro antiproliferative activity and kinase profile of new benzimidazole and benzotriazole derivatives

Konrad Chojnacki et al.

BIOORGANIC CHEMISTRY (2017)

Article Multidisciplinary Sciences

Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys

Travis K. Warren et al.

NATURE (2016)

Article Chemistry, Multidisciplinary

SYNTHESIS AND ANTIBACTERIAL EVALUATION OF SOME NOVEL MANNICH BASES OF BENZIMIDAZOLE DERIVATIVES

A. Ahmadi

BULLETIN OF THE CHEMICAL SOCIETY OF ETHIOPIA (2016)

Article Engineering, Electrical & Electronic

Octahydroacridine thin films grown by matrix-assisted pulsed laser evaporation for non linear optical applications

Valentin Ion et al.

MATERIALS SCIENCE IN SEMICONDUCTOR PROCESSING (2015)

Article Chemistry, Medicinal

Benzimidazole-1,2,3-triazole Hybrid Molecules: Synthesis and Evaluation for Antibacterial/Antifungal Activity

Abdelaaziz Ouahrouch et al.

ARCHIV DER PHARMAZIE (2014)

Article Chemistry, Medicinal

Part I. Synthesis, biological evaluation and docking studies of new 2-furylbenzimidazoles as antiangiogenic agents

Ahmed Temirak et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Chemistry, Medicinal

Benzimidazole clubbed with triazolo-thiadiazoles and triazolo-thiadiazines: New anticancer agents

Asif Husain et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Chemistry, Medicinal

Discovery of highly potent triazole antifungal derivatives by heterocycle-benzene bioisosteric replacement

Zhigan Jiang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Chemistry, Multidisciplinary

Synthesis and Pharmacological Evaluation of Some Novel 2-Mercapto Benzimidazole Derivatives

Sidram A. Nevade et al.

JOURNAL OF THE KOREAN CHEMICAL SOCIETY-DAEHAN HWAHAK HOE JEE (2013)

Article Chemistry, Medicinal

Benzimidazole bearing oxadiazole and triazolo-thiadiazoles nucleus: Design and synthesis as anticancer agents

Asif Husain et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2012)

Article Chemistry, Multidisciplinary

Synthesis and biological activity of some triazole-bearing benzimidazole derivatives

K. F. Ansari et al.

JOURNAL OF THE SERBIAN CHEMICAL SOCIETY (2011)

Article Chemistry, Medicinal

SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents

Ganesh Rajaram Jadhav et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2009)

Article Chemistry, Medicinal

Clubbed [1,2,3] triazoles by fluorine benzimidazole: A novel approach to H37Rv inhibitors as a potential treatment for tuberculosis

Charansingh Gill et al.

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2008)

Article Chemistry, Medicinal

A simple approach for indexing the oral druglikeness of a compound: Discriminating druglike compounds from nondruglike ones

Dhrubajyoti Biswas et al.

JOURNAL OF CHEMICAL INFORMATION AND MODELING (2006)

Article Biochemistry & Molecular Biology

Synthesis and antioxidant properties of novel benzimidazole derivatives

G Ayhan-Kilcigil et al.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY (2004)

Article Biochemistry & Molecular Biology

Synthesis and antimicrobial activity of some new benzimidazole derivatives

AH El-masry et al.

MOLECULES (2000)