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

Authors
Goker, H Ayhan-Kilcigil, G Tuncbilek, M Kus, C Ertan, R Kendi, E Ozbey, S Fort, M Garcia, C Farre, AJ
Citation
H. Goker et al., Synthesis and antihistaminic H-1 activity of 1,2,5(6)-trisubstituted benzimidazoles, HETEROCYCLE, 51(11), 1999, pp. 2561-2573
Citations number
21
Categorie Soggetti
Organic Chemistry/Polymer Science
Journal title
HETEROCYCLES
ISSN journal
03855414 → ACNP
Volume
51
Issue
11
Year of publication
1999
Pages
2561 - 2573
Database
ISI
SICI code
0385-5414(19991101)51:11<2561:SAAHAO>2.0.ZU;2-G
Abstract
A number of benzimidazoles, having several substituents on the azole and be nzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for th e 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-an tihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.