Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.

@article{Xu2007SynthesisAB,
  title={Synthesis and biological activity of 2-alkylbenzimidazoles bearing a N-phenylpyrrole moiety as novel angiotensin II AT1 receptor antagonists.},
  author={Jin Yi Xu and Yi Zeng and Qian Jiang Ran and Zhen Bo Wei and Yi Bi and Qian He and Qiu Juan Wang and Song Hu and Jing Zhang and Ming Yue Tang and Wei Yi Hua and Xiao Ming Wu},
  journal={Bioorganic & medicinal chemistry letters},
  year={2007},
  volume={17 10},
  pages={
          2921-6
        }
}
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. 
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