Synthesis and evaluation of in vitro anti-microbial and anti-tubercular activity of 2-styryl benzimidazoles

A new series of novel 5-(nitro/bromo)-styryl-2-benzimidazoles ( 1– 12) has been synthesized by simple, mild and efficient synthetic protocol by attempted condensation of 5-(nitro/bromo)- o-phenylenediamine with trans-cinnamic acids in ethylene glycol. Screening for in vitro anti-tubercular activity...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2009-10, Vol.44 (10), p.4244-4248
Main Authors: Shingalapur, Ramya V., Hosamani, Kallappa M., Keri, Rangappa S.
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Anti-microbial activity
Anti-tubercular activity
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antifungal agents
Antifungal Agents - chemical synthesis
Antifungal Agents - chemistry
Antifungal Agents - pharmacology
Antitubercular Agents - chemical synthesis
Antitubercular Agents - chemistry
Antitubercular Agents - pharmacology
Bacteria - drug effects
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Biological and medical sciences
Ethylene glycol
Fungi - drug effects
General aspects
Medical sciences
Microbial Sensitivity Tests
Mycobacterium tuberculosis - drug effects
Pharmacology. Drug treatments
Structure-Activity Relationship
Styryl benzimidazole
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Summary:A new series of novel 5-(nitro/bromo)-styryl-2-benzimidazoles ( 1– 12) has been synthesized by simple, mild and efficient synthetic protocol by attempted condensation of 5-(nitro/bromo)- o-phenylenediamine with trans-cinnamic acids in ethylene glycol. Screening for in vitro anti-tubercular activity against Mycobacterium tuberculosis H 37 Rv, anti-bacterial activity against Staphylococcus aureus, Escherichia coli, Enterococcus faecalis, Klebsiella pneumoniae bacterial strains and anti-fungal activity against Candida albicans and Asperigillus fumigatus fungal strains were carried out. Compounds 5, 7, 8, 9, 11 showed higher anti-tubercular activity and compounds 7, 8, 10, 11, 12 have proved to be effective with MIC (μg/ml) and emerged as lead molecules showing excellent activities against a panel of microorganisms. All synthesized compounds were characterized using IR, 1H, 13C NMR, GC–MS and elemental analysis. An efficient synthetic protocol for condensation of 5-(nitro/bromo)- o-phenylenediamine with trans-cinnamic acids to prepare novel 5-(nitro/bromo)-styryl-2-benzimidazole is obtained. The characterized compounds were screened for their in vitro anti-tubercular, anti-microbial and antifungal activities. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2009.05.021