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.
Mini-Reviews in Medicinal Chemistry
Title:The Progress Towards the Development of DHQO Derivatives and Related Analogues with Inotropic Effects
Volume: 13 Issue: 12
Author(s): Y. Wu and H.-R. Piao
Affiliation:
Keywords: Congestive heart failure, Positive inotropic activity, 3, 4-Dihydro-2(1H)-quinolinone, Vesnarinone, Structureactivity relationship.
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.
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Cite this article as:
Wu Y. and Piao H.-R., The Progress Towards the Development of DHQO Derivatives and Related Analogues with Inotropic Effects, Mini-Reviews in Medicinal Chemistry 2013; 13 (12) . https://dx.doi.org/10.2174/13895575113136660089
DOI https://dx.doi.org/10.2174/13895575113136660089 |
Print ISSN 1389-5575 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5607 |
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