title: The progress towards the development of DHQO derivatives and related analogues with inotropic effects.
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.
authors.affiliation: Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education; Yanbian University College of Pharmacy, Yanji 133000, PR China. piaohuri@yahoo.com.cn.
authors.forename: Y
authors.initials: Y
authors.lastname: Wu
authors.forename: H-R
authors.initials: HR
authors.lastname: Piao
mesh_terms: D000818:Animals; D002316:Cardiotonic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011719:Pyrazines; D011804:Quinolines / Q000737:chemistry; D015363:Quinolones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011817:Rabbits; D013318:Stroke Volume / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D002316:Cardiotonic Agents; D011719:Pyrazines; D011804:Quinolines; D015363:Quinolones; C041667:vesnarinone