SYNTHESIS AND MICROBIOLOGICAL ACTIVITY OF 5(OR 6)-METHYL-2-SUBSTITUTED BENZOXAZOLE AND BENZIMIDAZOLE DERIVATIVES

Citation
I. Oren et al., SYNTHESIS AND MICROBIOLOGICAL ACTIVITY OF 5(OR 6)-METHYL-2-SUBSTITUTED BENZOXAZOLE AND BENZIMIDAZOLE DERIVATIVES, Arzneimittel-Forschung, 47(12), 1997, pp. 1393-1397
Citations number
33
Journal title
ISSN journal
00044172
Volume
47
Issue
12
Year of publication
1997
Pages
1393 - 1397
Database
ISI
SICI code
0004-4172(1997)47:12<1393:SAMAO5>2.0.ZU;2-5
Abstract
The synthesis and microbiological activity of a new series of 5 (or 6) -methyl-2-substituted benzoxazoles (IVa-n) and benzimidazoles (Va-h) w ere described. The in vitro microbiological activity of the compounds was determined against gram-positive, gram-negative bacteria and the y east Candida albicans in comparison to reference drugs. Microbiologica l results indicated that the derivatives possessed a broad spectrum of activity against the tested microorganisms and the compounds IVa-g, I Vi-k, IVn, Vb-c and Vh showed significant activity against Pseudomonas aeruginosa having MIC values of 25 mu g/ml, providing higher potencie s than the reference drugs tetracycline and streptomycin. Moreover, th e derivative 5-methyl-2-(p-chlorobenzyl)benzoxazole (IVb) possessed th e same potency against Candida albicans as the reference drugs oxicona zole and haloprogin having a MIC value of 6.25 mg/ml. However, none of the derivatives showed a better spectrum of activity than the referen ce drugs.