Amidino benzimidazole inhibitors of bacterial two-component systems

被引:127
作者
Weidner-Wells, MA [1 ]
Ohemeng, KA [1 ]
Nguyen, VN [1 ]
Fraga-Spano, S [1 ]
Macielag, MJ [1 ]
Werblood, HM [1 ]
Foleno, BD [1 ]
Webb, GC [1 ]
Barrett, JF [1 ]
Hlasta, DJ [1 ]
机构
[1] RW Johnson Pharmaceut Res Inst, Drug Discovery, Raritan, NJ 08869 USA
关键词
D O I
10.1016/S0960-894X(01)00024-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Amidino benzimidazoles have been identified as inhibitors of the bacterial KinA/Spo0F two-component system (TCS). Many of these inhibitors exhibit good in vitro antibacterial activity against a variety of susceptible and resistant Gram-positive organisms. The moiety at the 2-position of the benzimidazole was extensively modified. In addition, the regioisomeric benzoxazoles, heterocyclic replacements for the benzimidazole, have been synthesized and their activity against the TCS evaluated. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1545 / 1548
页数:4
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