SYNTHESIS OF 1,2,5(6)-TRISUBSTITUTED BENZIMIDAZOLES AND EVALUATION OF THEIR ANTIMICROBIAL ACTIVITIES


GOKER H., KUS C., ABBASOGLU U.

ARCHIV DER PHARMAZIE, vol.328, no.5, pp.425-430, 1995 (Journal Indexed in SCI) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 328 Issue: 5
  • Publication Date: 1995
  • Doi Number: 10.1002/ardp.19953280506
  • Title of Journal : ARCHIV DER PHARMAZIE
  • Page Numbers: pp.425-430

Abstract

A series of 22 benzimidazoles, having several substituents on the azole and benzene nuclei, were prepared and evaluated in vitro for antimicrobial activity. At first 2-chloro or 2-chloromethyl-5(6)-substituted-1H-benzimidazoles were synthesized, which were then substituted at C-2 with several piperazine or piperidine derivatives. The antibacterial activity of these compounds against Staphylococcus aureus, Bacillus subtilis, Escherichia coli and Pseudomonas aeruginosa, and the antifungal activity against Candida albicans, Candida stellatoidea, Candida parapsilosis, and Candida pseudotropicalis were determined as the MIC values. Since compound 12 exhibits good activity, in order to clarify the effect of substituents at C-1 on the activity, benzimidazole derivatives having ethyl, allyl, benzyl, and p-fluorobenzyl substituents at C-1 were prepared, and slightly increased activity was seen.