Amidino benzimidazoles have been identified as inhibitors of the bacterial
KinA/Spo0F two-component system (TCS). Many of these inhibitors exhibit goo
d in vitro antibacterial activity against a variety of susceptible and resi
stant Gram-positive organisms. The moiety at the 2-position of the benzimid
azole was extensively modified. In addition, the regioisomeric benzoxazoles
, heterocyclic replacements for the benzimidazole, have been synthesized an
d their activity against the TCS evaluated. (C) 2001 Elsevier Science Ltd.
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