Design, synthesis, and biological evaluation of 1,2,4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates

Jie Liu, Qin Liu, Xue Yang, Shengtao Xu, Hengyuan Zhang, Renren Bai, Hequan Yao, Jieyun Jiang, Mingqin Shen, Xiaoming Wu, Jinyi Xu

Research output: Contribution to journalArticlepeer-review

37 Scopus citations

Abstract

A series of novel 1,2,4-triazole bearing 5-substituted biphenyl-2- sulfonamide derivatives were designed and synthesized to develop new angiotensin II subtype 2 (AT2) receptor agonists as novel antihypertensive candidates. It was found that 14f (IC50 = 0.4 nM) and 15e (IC 50 = 5.0 nM) displayed potent AT2 receptor affinity and selectivity in binding assays. Biological evaluation in vivo suggested that 14f is obviously superior to that of reference drug losartan in RHRs, and meanwhile, 14f has no significant impact on heart rate. The interesting activities of these compounds may make them promising candidates as antihypertensive agents.

Original languageEnglish
Pages (from-to)7742-7751
Number of pages10
JournalBioorganic and Medicinal Chemistry
Volume21
Issue number24
DOIs
StatePublished - Dec 15 2013

Bibliographical note

Funding Information:
This study was financially supported by a grant from National Natural Science Fund (No. 81302635 ) and Project Program of State Key Laboratory of Natural Medicines, China Pharmaceutical University ( JKGQ201115 ).

Keywords

  • AT receptor
  • Agonists
  • Antihypertensive activity
  • Biphenyl-2-sulfonamide derivatives
  • Structure-activity relationships

ASJC Scopus subject areas

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

Fingerprint

Dive into the research topics of 'Design, synthesis, and biological evaluation of 1,2,4-triazole bearing 5-substituted biphenyl-2-sulfonamide derivatives as potential antihypertensive candidates'. Together they form a unique fingerprint.

Cite this