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 ,
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
