Novel hybrids of natural isochroman-4-one bearing N-substituted isopropanolamine as potential antihypertensive candidates

Renren Bai, Xiaojing Huang, Xue Yang, Wen Hong, Yiqun Tang, Hequan Yao, Jieyun Jiang, Jie Liu, Mingqin Shen, Xiaoming Wu, Jinyi Xu

Research output: Contribution to journalArticlepeer-review

10 Scopus citations


A series of novel hybrids of natural isochroman-4-one bearing isopropanolamine moiety were designed, synthesized and evaluated for their antihypertensive activity. It was found that compound IIId, prepared by hybridizing N-isopropyl substituted isopropanolamine functionality to a phenolic oxygen of isochroman-4-one, exhibited potent β1-adrenoceptor blocking effect comparable to the well-known antihypertensive drug propranolol. Additionally, IIId significantly reduced the systolic and diastolic blood pressure in SHRs by over 40%, which was obviously stronger than the lead compounds 7,8-dihydroxy-3-methyl-isochroman-4-one (XJP) and its analogue XJP-B. Overall, IIId may be a promising antihypertensive candidate for further investigation.

Original languageEnglish
Pages (from-to)2495-2502
Number of pages8
JournalBioorganic and Medicinal Chemistry
Issue number9
StatePublished - May 1 2013

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 ).

Copyright 2013 Elsevier B.V., All rights reserved.


  • Antihypertensive activity
  • Hybrids
  • Isochroman-4-one
  • Isopropanolamine
  • β-Adrenoceptor blockers

ASJC Scopus subject areas

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


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