title: Design, synthesis, and evaluation of 5-sulfamoyl benzimidazole derivatives as novel angiotensin II receptor antagonists.
abstract: A series of 5-alkylsulfamoyl benzimidazole derivatives have been designed and synthesized as novel angiotensin II (Ang II) receptor antagonists. The compounds have been evaluated for in vitro Ang II antagonism and for in vivo antihypertensive activity on isolated rat aortic ring and desoxycortisone acetate induced hypertensive rats, respectively. The activity is found related to size of alkyl group. The maximum activity is observed with a compact and bulky alkyl group like tert-butyl and cyclohexyl. The compounds 4g and 4h have shown promising both in vitro and in vivo activities. A receptor binding model is also proposed on the basis on the basis of structure-activity relationship in this study.
authors.affiliation: Department of Pharmaceutical Sciences and Drug Research, Punjabi University, Patiala, Punjab 147002, India.
authors.forename: Navneet
authors.initials: N
authors.lastname: Kaur
authors.forename: Amardeep
authors.initials: A
authors.lastname: Kaur
authors.forename: Yogita
authors.initials: Y
authors.lastname: Bansal
authors.forename: Dhvanit I
authors.initials: DI
authors.lastname: Shah
authors.forename: Gulshan
authors.initials: G
authors.lastname: Bansal
authors.forename: Manjeet
authors.initials: M
authors.lastname: Singh
mesh_terms: D057912:Angiotensin II Type 2 Receptor Blockers; D000818:Animals; D000959:Antihypertensive Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001794:Blood Pressure / Q000502:physiology; D015195:Drug Design; D051381:Rats; D044139:Receptor, Angiotensin, Type 2 / Q000378:metabolism
chemical_list: D057912:Angiotensin II Type 2 Receptor Blockers; D000959:Antihypertensive Agents; D001562:Benzimidazoles; D044139:Receptor, Angiotensin, Type 2