Title of article
Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists
Author/Authors
Jin Yi Xu، نويسنده , , Yi Zeng، نويسنده , , Qian Ran، نويسنده , , Zhen Wei، نويسنده , , Yi Bi، نويسنده , , Qian Hui He، نويسنده , , Qiu Juan Wang، نويسنده , , Song Hu، نويسنده , , Jing Zhang، نويسنده , , Ming Yue Tang، نويسنده , , Wei Yi Hua، نويسنده , , Xiao Ming Wu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
6
From page
2921
To page
2926
Abstract
A series of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety were synthesized and evaluated as a novel class of AT1 receptor antagonists. Among them, compounds 10a and 10g inhibited [125I] AngII-binding affinity to AT1 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 AT1 receptor antagonist.
Keywords
AT1 receptor antagonists , synthesis , activity , hypertension , 2-Alkylbenzimidazole
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
798150
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