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Bioorg Med Chem Lett. 2001 Jun 18;11(12):1545-8.

Amidino benzimidazole inhibitors of bacterial two-component systems.

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Drug Discovery, The R. W. Johnson Pharmaceutical Research Institute, 1000 Route 202, Raritan, NJ 08869, USA.


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.

[Indexed for MEDLINE]

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