Synthesis and biological evaluation of 4′-[(benzimidazole-1-yl) methyl] biphenyl-2-sulfonamide derivatives as dual angiotensin II/endothelin A receptor antagonists

R Bai, Z Wei, J Liu, W Xie, H Yao, X Wu, J Jiang…

Index: Bai, Renren; Wei, Zhen; Liu, Jie; Xie, Weijia; Yao, Hequan; Wu, Xiaoming; Jiang, Jieyun; Wang, Qiujuan; Xu, Jinyi Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 15 p. 4661 - 4667

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Citation Number: 12

Abstract

A series of 4′-[(benzimidazole-1-yl) methyl] biphenyl-2-sulfonamide derivatives (Ia–Il) were synthesized and biologically evaluated. It was found that Ig, the most active compound, antagonized both Ang II AT1 and endothelin ETA receptors (AT1 IC50= 8.5, ETA IC50= 8.9 nM), and was more potent than losartan in RHRs with no significant effect on heart rate. The preliminary structure–activity relationships were also discussed in the present paper.