The chemistry of pseudomonic acid .15. Synthesis and antibacterial activity of a series of 5-alkyl, 5-alkenyl, and 5-heterosubstituted oxazoles

被引:43
作者
Brown, P
Davies, DT
OHanlon, PJ
Wilson, JM
机构
[1] SmithKline Beecham Pharmaceuticals, Betckworth, Surrey, RH3 7AJ, Brockham Park
关键词
D O I
10.1021/jm9503862
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a range of 5-alkyl, 5-alkenyl, and 5-heterosubstituted 2-(1-normon-2-yl) oxazoles is described. The antibacterial activity was determined as the minimum inhibitory concentration against a range of Gram-positive and Gram-negative organisms using a standard Agar dilution procedure. Compounds possessing an acid functionality directly on, or close to, the ring were found to be of greatly decreased potency, while increasing lipophilicity with greater chain length led to increased potency of these derivatives.
引用
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页码:446 / 457
页数:12
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