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Mini-Reviews in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1389-5575
ISSN (Online): 1875-5607

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

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

Volume 13, Issue 12, 2013

Page: [1801 - 1811] Pages: 11

DOI: 10.2174/13895575113136660089

Price: $65

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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