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., ...Daha Fazla

HETEROCYCLES, cilt.51, sa.11, ss.2561-2573, 1999 (SCI-Expanded) identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 51 Sayı: 11
  • Basım Tarihi: 1999
  • Dergi Adı: HETEROCYCLES
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.2561-2573
  • Hacettepe Üniversitesi Adresli: Evet

Özet

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.