Synthesis and antihistaminic H-1 activity of 1,2,5(6)-trisubstituted benzimidazoles

GOKER H., AYHAN-KILCIGIL G., TUNCBILEK M. G., KUS C., ERTAN R., KENDI E., ...More

HETEROCYCLES, vol.51, no.11, pp.2561-2573, 1999 (SCI-Expanded) identifier

  • Publication Type: Article / Article
  • Volume: 51 Issue: 11
  • Publication Date: 1999
  • Journal Name: HETEROCYCLES
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.2561-2573
  • Hacettepe University Affiliated: Yes

Abstract

A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N-1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H-1-antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.