The chemistry of pseudomonic acid. Part 14. Synthesis and in vivo biological activity of heterocyclyl substituted oxazole derivatives.
作者信息
Broom N J, Elder J S, Hannan P C, Pons J E, O'Hanlon P J, Walker G, Wilson J, Woodall P
机构信息
SmithKline Beecham Pharmaceuticals, Brockham Park, Betchworth, Surrey.
出版信息
J Antibiot (Tokyo). 1995 Nov;48(11):1336-44. doi: 10.7164/antibiotics.48.1336.
PMID:8557577
Abstract
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.
摘要
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