细菌双组分系统的脒基苯并咪唑抑制剂。
Amidino benzimidazole inhibitors of bacterial two-component systems.
作者信息
Weidner-Wells M A, Ohemeng K A, Nguyen V N, Fraga-Spano S, Macielag M J, Werblood H M, Foleno B D, Webb G C, Barrett J F, Hlasta D J
机构信息
Drug Discovery, The R. W. Johnson Pharmaceutical Research Institute, 1000 Route 202, Raritan, NJ 08869, USA.
出版信息
Bioorg Med Chem Lett. 2001 Jun 18;11(12):1545-8. doi: 10.1016/s0960-894x(01)00024-5.
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.
脒基苯并咪唑已被确定为细菌KinA/Spo0F双组分系统（TCS）的抑制剂。其中许多抑制剂对多种敏感和耐药革兰氏阳性菌表现出良好的体外抗菌活性。苯并咪唑2位的部分被广泛修饰。此外，已经合成了苯并恶唑的区域异构体，即苯并咪唑的杂环替代物，并评估了它们对TCS的活性。
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