Synthesis and structure-activity relationships of novel THF 1 beta-methylcarbapenems

被引:15
作者
Lin, YI
Bitha, P
Sakya, SM
Strohmeyer, TW
Li, Z
Lee, VJ
Lang, SA
Yang, YJ
Bhachech, N
Weiss, WJ
Petersen, PJ
Jacobus, NV
Bush, K
Testa, RT
Tally, FP
机构
[1] Wyeth-Ayerst Research, Div. of Amer. Home Prod. Corporation, Infectious Diseases Research Section, Pearl River
关键词
D O I
10.1016/S0960-894X(97)00282-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of twelve highly active aminomethyl-THF 1 beta-methylcarbapenems 3a-1 were synthesized. Of these, carbapenems 3a-f demonstrated a spectrum of antimicrobial activity comparable to those of imipenem and meropenem with the exception of only moderate anti-pseudomonal activity. Most importantly, they demonstrated moderate intrinsic oral activity against an E. coli infection in mice. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:1671 / 1676
页数:6
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