Novel benzimidazole-4-carboxylic acid derivatives as potent and selective 5-HT 3 receptor ligands

ML López-Rodríguez, MJ Morcillo, B Benhamú…

Index: Lopez-Rodriguez, Maria L.; Morcillo, Ma Jose; Benhamu, Bellinda; Riaguas, Ma Dolores Bioorganic and Medicinal Chemistry Letters, 1996 , vol. 6, # 11 p. 1195 - 1198

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Citation Number: 11

Abstract

A series of benzimidazole-4-carboxylic acid derivatives was synthesized and evaluated for affinity at 5-HT3 and 5-HT4 serotoninergic receptors. Compounds 1b, c and j exhibited high affinity for the 5-HT3 receptors (Ki= 6.1, 3.7 and 4.9 nM, respectively) and no significant affinity for 5-HT4 (Ki> 1000 nM) and 5-HT1A (Ki> 10 000 nM) sites. Preliminary studies showed that 1c displayed activity in the two-compartment behavioural model.