THE CHEMISTRY OF PSEUDOMONIC ACID .14. SYNTHESIS AND IN-VIVO BIOLOGICAL-ACTIVITY OF HETEROCYCLYL SUBSTITUTED OXAZOLE DERIVATIVES

被引:31
作者
BROOM, NJP [1 ]
ELDER, JS [1 ]
HANNAN, PCT [1 ]
PONS, JE [1 ]
OHANLON, PJ [1 ]
WALKER, G [1 ]
WILSON, J [1 ]
WOODALL, P [1 ]
机构
[1] SMITHKLINE BEECHAM PHARMACEUT,BETCHWORTH RH3 7AJ,SURREY,ENGLAND
关键词
D O I
10.7164/antibiotics.48.1336
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
Semisynthetic analogues of pseudomonic, acid A have been prepared containing a heterocyclyl substituted oxazole. Derivatives in which the heterocycle was thiophene, furan, pyridine, or isoxazole showed good antibacterial potency and were further evaluated in vivo. Both pharmacokinetic parameters and oral activity against an experimental intraperitoneal sepsis were superior to results obtained from previously described pseudomonic acid A derivatives.
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收藏
页码:1336 / 1344
页数:9
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