Synthesis and microbiological activity of some novel 5- or 6-methyl-2-(2,4-disubstituted phenyl) benzoxazole derivatives.

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作者：

O Temiz，I Oren，E Sener，I Yalçin，N Uçartürk

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摘要：

The synthesis of a new series of 5- or 6-methyl-2-(2,4-disubstituted phenyl)benzoxazoles ( 4, 5 ) is described in order to determine their antimicrobial activities and feasible structure-activity relationships. The synthesized compounds were tested in vitro against three Gram-positive bacteria, three Gram-negative bacteria and the yeast Candida albicans , in comparison with several control drugs. Microbiological results exhibited that the synthesized compounds possess a broad spectrum of antibacterial activity against the tested microorganisms. The compounds 4b and 4c indicated some antibacterial activity against Staphylococcus aureus having a minimum inhibitory concentration (MIC) of 12.5 μg/ml. Moreover, the compound 5a revealed a significant antibacterial activity against the enterobacter Pseudomonas aeruginosa showing a MIC value of 25 μg/ml, i.e. more potent than the control drugs tetracycline and streptomycin. For the antimycotic activity against the yeast C. albicans , the derivative 4c was found to be more active than the other synthesized compounds with a MIC value of 12.5 μg/ml, but one-fold less potent than the control drugs oxiconazole and haloprogin.

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关键词：

benzoxazole derivatives ring closure reactions pharmacology, medicinal chemistry, vaccines, serums

DOI：

10.1016/S0014-827X(98)00030-5

被引量：

254

年份：

1998