Literature DB >> 17412584

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

Jin Yi Xu1, Yi Zeng, Qian Ran, Zhen Wei, Yi Bi, Qian Hui He, Qiu Juan Wang, Song Hu, Jing Zhang, Ming Yue Tang, Wei Yi Hua, Xiao Ming Wu.   

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.

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Year:  2007        PMID： 17412584     DOI： 10.1016/j.bmcl.2007.02.042

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  2 in total

1.  Conventional and microwave-assisted synthesis of new indole-tethered benzimidazole-based 1,2,3-triazoles and evaluation of their antimycobacterial, antioxidant and antimicrobial activities.

Authors:  Dongamanti Ashok; Srinivas Gundu; Vikas Kumar Aamate; Mohan Gandhi Devulapally
Journal:  Mol Divers       Date:  2018-04-18       Impact factor: 2.943

2.  Design, synthesis, biological assessment and in silico ADME prediction of new 2-(4-(methylsulfonyl) phenyl) benzimidazoles as selective cyclooxygenase-2 inhibitors.

Authors:  Mohamed A S Badawy; Eman K A Abdelall; El-Shaymaa El-Nahass; Khaled R A Abdellatif; Hamdy M Abdel-Rahman
Journal:  RSC Adv       Date:  2021-08-17       Impact factor: 4.036
  2 in total

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