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
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.