Synthesis and antihistaminic H1 activity of 1,2,5(6)-trisubstituted benzimidazoles

GÖKER A. H., Ayhan-Kilcigil G., TUNÇBİLEK M., KUŞ 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
  • Doi Number: 10.3987/com-99-8585
  • Journal Name: Heterocycles
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.2561-2573
  • Ankara 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 N1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H1- antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.