Angiotensin II – AT1 receptor antagonists: Design, synthesis and evaluation of substituted carboxamido benzimidazole derivatives

• DOI: 10.1016/j.ejmech.2007.11.008
• Publication Date: 2007-11-26T10:22:09Z
• Authors: Dhvanit I. Shah; Manu Sharma; Yogita Bansal; Gulshan Bansal; Manjeet Singh
• Keywords: Reference Standards; 01 natural sciences; Receptor, Angiotensin, Type 1; Rats; 0104 chemical sciences; 3. Good health; Drug Design; Hypertension; Animals; Benzimidazoles; Angiotensin II Type 1 Receptor Blockers; Antihypertensive Agents

A series of 5-(alkyl and aryl)carboxamido benzimidazole derivatives had been designed, synthesized and evaluated for in vitro angiotensin II--AT1 receptor antagonism and in vivo antihypertensive activities. The pharmacological activities were inversely related to the size of alkyl and aryl substituents. It can be suggested that compounds with lower alkyl groups at 5-position of benzimidazole nucleus demonstrated potent antihypertensive activity.