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

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

  • Bioorg Med Chem. 2012 Aug 1;20(15):4661-7. doi: 10.1016/j.bmc.2012.06.011.
Renren Bai 1,  Zhen Wei,  Jie Liu,  Weijia Xie,  Hequan Yao,  Xiaoming Wu,  Jieyun Jiang,  Qiujuan Wang,  Jinyi Xu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, PR China.
PMID: 22750010 DOI: 10.1016/j.bmc.2012.06.011
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 AT(1) and endothelin ET(A) receptors (AT(1) IC(50)=8.5, ET(A) IC(50)=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.

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