Novel nitric oxide-releasing isochroman-4-one derivatives: Synthesis and evaluation of antihypertensive activity

Renren Bai, Xue Yang, Yao Zhu, Zhiwen Zhou, Weijia Xie, Hequan Yao, Jieyun Jiang, Jie Liu, Mingqin Shen, Xiaoming Wu, Jinyi Xu

Research output: Contribution to journalArticlepeer-review

25 Scopus citations


By coupling nitric oxide (NO)-donor moieties with a natural antihypertensive product (±)-7,8-dihydroxy-3-methyl-isochroman-4-one [(±)-XJP] and its analogue (±)-XJP-B, a series of novel NO-releasing isochroman-4-one derivatives were designed and synthesized. The NO-releasing assay indicated that compounds Ia, Id, IIIb and IIIe released the maximum amount of NO. The maximum reductions of blood pressure of Ia, IIIb and IIIe in SHRs were nearly 40%, which was obviously superior to that of the lead compounds and comparable to that of reference drug captopril. These results suggested that NO-donor/natural product hybrids may provide a promising approach for the discovery of novel antihypertensive agents.

Original languageEnglish
Pages (from-to)6848-6855
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number23
StatePublished - Dec 1 2012

Bibliographical note

Funding Information:
This study was financially supported by a grant from ‘Eleventh Five-Year’ Major Innovation Projects for New Drug Candidates (No. 2009ZX09103-128), Project for Research and Innovation of Graduates in Colleges and Universities of Jiangsu Province (CXZZ11-0798), Fundamental Research Funds for the Central Universities (JKY2011027) and Project Program of State Key Laboratory of Natural Medicines, China Pharmaceutical University (JKGQ201115).


  • Antihypertensive activity
  • Hybrids
  • Isochroman-4-one derivatives
  • Nitric oxide (NO)
  • Structure modification

ASJC Scopus subject areas

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


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