NOVEL BENZIMIDAZOLE-4-CARBOXYLIC ACID-DERIVATIVES AS POTENT AND SELECTIVE 5-HT3 RECEPTOR LIGANDS

Authors
LOPEZRODRIGUEZ ML MORCILLO MJ BENHAMU B RIAGUAS MD
Citation
Ml. Lopezrodriguez et al., NOVEL BENZIMIDAZOLE-4-CARBOXYLIC ACID-DERIVATIVES AS POTENT AND SELECTIVE 5-HT3 RECEPTOR LIGANDS, Bioorganic & medicinal chemistry letters, 6(11), 1996, pp. 1195-1198
Citations number
19
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
11
Year of publication
1996
Pages
1195 - 1198
Database
ISI
SICI code
0960-894X(1996)6:11<1195:NBAAPA>2.0.ZU;2-S
Abstract
A series of benzimidazole-4-carboxylic acid derivatives was synthesize d and evaluated for affinity at 5-HT3 and 5-HT4 serotoninergic recepto rs. Compounds 1b, c and j exhibited high affinity for the 5-HT3 recept ors (K-i=6.1, 3.7 and 4.9 nM, respectively) and no significant affinit y for 5-HT4 (K-i>1000 nM) and 5-HT1A (K-i>10 000 nM) sites. Preliminar y studies showed that 1c displayed activity in the two-compartment beh avioural model. Copyright (C) 1996 Elsevier Science Ltd