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Eur J Med Chem ; 44(7): 2930-5, 2009 Jul.
Article in English | MEDLINE | ID: mdl-19150154

ABSTRACT

In the present study, a series of novel 2-[4-(1H-[1,2,4]-triazol-1-yl)phenyl]-1-substituted-4,6-difluoro-1H-benzo[d]imidazole derivatives are synthesized by the alkylation of 2-[4-(1H-[1,2,4]-triazol-1-yl)phenyl]-4,6-difluoro-1H-benzo[d]imidazole with substituted alkyl and aryl halides. The compounds were evaluated for their preliminary in-vitro antibacterial activity against Pseudomonas aeruginosa, Escherichia coli, Staphylococcus aureus, and Salmonella typhosa and then were screened for their antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth microdilution assay method. The antibacterial data suggested that the analogs with electronegative substituents emerged as promising antimicrobials. It was also observed that the promising antimicrobials have proved to be better antimycobacterials. Few of selected analogs are under further evaluation for secondary antitubercular screening, as they have shown better activity compared to rifampin.


Subject(s)
Anti-Infective Agents/chemistry , Anti-Infective Agents/pharmacology , Benzimidazoles/chemistry , Benzimidazoles/pharmacology , Mycobacterium tuberculosis/drug effects , Triazoles/chemistry , Anti-Infective Agents/chemical synthesis , Antitubercular Agents/chemical synthesis , Antitubercular Agents/chemistry , Antitubercular Agents/pharmacology , Benzimidazoles/chemical synthesis , Structure-Activity Relationship
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