title: Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.
abstract: A series of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety were synthesized and evaluated as a novel class of AT(1) receptor antagonists. Among them, compounds 10a and 10g inhibited [(125)I] AngII-binding affinity to AT(1) receptor at nanomolar level and potently inhibited the Ang II-induced pressor response by oral administration. Moreover, evaluation in spontaneously hypertensive rats showed that 10a is an orally active AT(1) receptor antagonist.
authors.affiliation: Department of Medicinal Chemistry, College of Pharmacy, China Pharmaceutical University, 24 Tongjia Xiang, Nanjing 210009, China. jinyixu@china.com
authors.forename: Jin Yi
authors.initials: JY
authors.lastname: Xu
authors.forename: Yi
authors.initials: Y
authors.lastname: Zeng
authors.forename: Qian
authors.initials: Q
authors.lastname: Ran
authors.forename: Zhen
authors.initials: Z
authors.lastname: Wei
authors.forename: Yi
authors.initials: Y
authors.lastname: Bi
authors.forename: Qian Hui
authors.initials: QH
authors.lastname: He
authors.forename: Qiu Juan
authors.initials: QJ
authors.lastname: Wang
authors.forename: Song
authors.initials: S
authors.lastname: Hu
authors.forename: Jing
authors.initials: J
authors.lastname: Zhang
authors.forename: Ming Yue
authors.initials: MY
authors.lastname: Tang
authors.forename: Wei Yi
authors.initials: WY
authors.lastname: Hua
authors.forename: Xiao Ming
authors.initials: XM
authors.lastname: Wu
mesh_terms: D000284:Administration, Oral; D047228:Angiotensin II Type 1 Receptor Blockers / Q000138:chemical synthesis* / Q000494:pharmacology*; D000818:Animals; D008958:Models, Molecular; D015394:Molecular Structure; D051381:Rats; D011918:Rats, Inbred SHR; D013329:Structure-Activity Relationship
chemical_list: D047228:Angiotensin II Type 1 Receptor Blockers