Anti-microbial benzimidazole derivatives: synthesis and in vitro biological evaluation

Soni, Love Kumar; Narsinghani, Tamanna; Sethi, Anand Kumar

doi:10.1007/s00044-012-9976-2

Cited by 16 publications

(9 citation statements)

References 19 publications

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“…Styryl benzimidazole derivatives reported as antimicrobial agents. Compounds 33 ( a , b ) showed higher activity against S. aureus, E. coli, and C. albicans with 72–93% inhibition . Trifluoromethyl benzimidazole derivatives were synthesized and tested for antimicrobial activity.…”

Section: Antimicrobial Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Benzimidazole‐Based Medicinal Chemistry

et al. 2014

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The properties of benzimidazole and its derivatives have been studied over more than one hundred years. Benzimidazole derivatives are useful intermediates/subunits for the development of molecules of pharmaceutical or biological interest. Substituted benzimidazole derivatives have found applications in diverse therapeutic areas such as antiulcer, anticancer agents, and anthelmintic species to name just a few. This work systematically gives a comprehensive review in current developments of benzimidazole-based compounds in the whole range of medicinal chemistry as anticancer, antibacterial, antifungal, anti-inflammatory, analgesic agents, anti-HIV, antioxidant, anticonvulsant, antitubercular, antidiabetic, antileishmanial, antihistaminic, antimalarial agents, and other medicinal agents. This review will further be helpful for the researcher on the basis of substitution pattern around the nucleus with an aim to help medicinal chemists for developing an SAR on benzimidazole drugs/compounds.

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Section: Antimicrobial Agentsmentioning

confidence: 99%

Comprehensive Review in Current Developments of Benzimidazole‐Based Medicinal Chemistry

et al. 2014

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“…They are effective against a wide range of diseases [5,6] . Many benzimidazole analogues have been reported to have antioxidant activity, [7–10] as well as antimicrobial activity [11–20] …”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, Antimicrobial Evaluation, Antioxidant Studies, and Molecular Docking of Some New 1H‐Benzimidazole Derivatives

et al. 2023

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The goal of this study is to synthesize and test a series of novel benzimidazole derivatives (3 a–3 q, 4 a, 4 b) for antimicrobial and antioxidant activity. The compounds were tested for antimicrobial activity in vitro using the macro dilution broth method. The antioxidant activity of the synthesized compounds was evaluated using assay of Lipid peroxidation (LP) level by measuring the formation of 2‐thiobarbituric acid reactive substances (TBARS) and 7‐Ethoxyresorufin O‐deethylase (EROD) activity. Only the compound 3 m demonstrated significant antimicrobial activity against all of the microorganisms tested. The LP level of compound 3 m (5.20±0.28, 68 %) was comparable to that of standard BHT (5.68±0.22, 65 %). Compounds 3 i (11 %, 28 %) and 3 m (13 %, 32 %) are the most active compounds on microsomal EROD activity and LP levels which are better than standard caffeine (15 %) and BHT (35 %), respectively. Also compounds 3 g (20 %), and 4 b (28 %) have much better LP levels than BHT (35 %). Compound 3 m exhibited high docking energies scores comparing with reference drugs when docked with bacterial Penicillin‐Binding Protein 3 and 4, sterol 14 α‐demethylase of C. albicans and urate oxidase enzyme.

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“…Heterocyclics, bi-cyclic scaffolds, or hybridized compounds formed by the fusion of a heterocyclic scaffold with another molecule have shown better therapeutic activity than their parents, leading to their popularity in modern chemotherapeutics. Benzimidazole scaffold has offered several biological activities like anticancer, 2 antimicrobial, 3 anti-inflammatory, 4 antimalarial, 5 antihypertensive, 6 etc. Several marketed drugs such as albendazole, mebendazole, tiabendazole, fenbendazole, lansoprazole, omeprazole, atacand, telmisartan, candesartan, mizolastine, bilastine, etc.…”

Section: Introductionmentioning

confidence: 99%

N-(2-(1H-benzo[d]imidazol-2-yl)Phenyl)-2- (Substituted-styryl)Aniline as Anti-proliferative Agents: Rejuvenating the Importance of Low Molecular Weight Ligands in Oncotherapeutics

Chhajed¹,

Gupta²,

Kshirsagar³

et al. 2020

IJPER

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Background:The rationale behind the study involved that in individuality benzimidazolebased molecules demonstrates significant anti-proliferative activity; chalcone molecules like xanthohumol are known to express noteworthy anti-cancer activity; benzamide derived products show remarkable inhibition of HDAC (an emerging anti-proliferative target) and styrene-based compounds possesses notable anti-tumor activity. Materials and Methods: In this research, an attempt was made to synthesize and characterize a series of hybridized molecules of the prototype (E)-N-(2-(1H-benzo[d]imidazol-2-yl) phenyl)-2-(substituted-styryl)aniline which comprises of a benzimidazole function; along with a chalcone (or styryl) moiety linked by a benzamide. The study involved screening of the novel derivatives against non-small cell lung cancer cell line (H460; ATCC: HTB177) and human colorectal cancer cell line (HCT116; ATCC: CCL-247) using Propidium Iodide assay. In silico docking study was also performed against protein tyrosine kinase (PDB ID: 2J5F) to determine the probable mechanism of action of the novel compounds. Results: The study reflected the profound role and positions of substitution on the phenyl moiety of the benzimidazole system. The compound DSTYR4 displayed most potent antiproliferative activity with IC 50 values of 2.98 μM against HCT116 cell line and 5.15 μM against H460 cell line. Conclusion: The research fruitfully rejuvenates the potentials and importance of small molecular weight ligands for experimental oncology.

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Anti-microbial benzimidazole derivatives: synthesis and in vitro biological evaluation

Cited by 16 publications

References 19 publications

Comprehensive Review in Current Developments of Benzimidazole‐Based Medicinal Chemistry

Comprehensive Review in Current Developments of Benzimidazole‐Based Medicinal Chemistry

Design, Synthesis, Antimicrobial Evaluation, Antioxidant Studies, and Molecular Docking of Some New 1H‐Benzimidazole Derivatives

N-(2-(1H-benzo[d]imidazol-2-yl)Phenyl)-2- (Substituted-styryl)Aniline as Anti-proliferative Agents: Rejuvenating the Importance of Low Molecular Weight Ligands in Oncotherapeutics

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