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

Renren Bai, Zhen Wei, Jie Liu, Weijia Xie, Hequan Yao, Xiaoming Wu, Jieyun Jiang, Qiujuan Wang, Jinyi Xu

Research output: Contribution to journalArticlepeer-review

24 Scopus citations

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.

Original languageEnglish
Pages (from-to)4661-4667
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume20
Issue number15
DOIs
StatePublished - Aug 1 2012

Bibliographical note

Funding Information:
This study was financially supported by grant from ‘Eleventh Five-Year’ Major Innovation Projects for New Drug Candidates (No. 2009ZX09102-036), Jiangsu Provincial Science Fund (No. BK2008344) and Project for Research and Innovation of Graduates in Colleges and Universities of Jiangsu Province (CXZZ11-0798).

Keywords

  • AT receptor
  • Antihypertensive activity
  • DARAs
  • ET receptor
  • Structure-activity relationships

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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