The Progress Towards the Development of DHQO Derivatives and Related Analogues with Inotropic Effects

Author(s): Y. Wu, H.-R. Piao.

Journal Name: Mini-Reviews in Medicinal Chemistry

Volume 13 , Issue 12 , 2013

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Abstract:

During the course of the past two decades, our group has worked towards the development of increasingly potent inotropic agents by making structural modifications to compounds derived from 3,4-dihydro-2(1H)-quinolinone (DHQO) and related analogues. Herein, we describe the design and synthesis of a new series of DHQO derivatives and the subsequent evaluation of their positive inotropic activity towards left atrium stroke volume in isolated rabbit-heart preparations. Some of these derivatives presented favorable in vitro activities compared with the reference drug, milrinone, and compound 10a, in particular is currently being investigated as a preclinical drug candidate. This review also describes our progress towards the development of DHQO derivatives and related analogues with positive inotropic activities from 1999 to 2013.

Keywords: Congestive heart failure, Positive inotropic activity, 3, 4-Dihydro-2(1H)-quinolinone, Vesnarinone, Structureactivity relationship.

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Article Details

VOLUME: 13
ISSUE: 12
Year: 2013
Page: [1801 - 1811]
Pages: 11
DOI: 10.2174/13895575113136660089
Price: $58

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