Cardiotonic agents. 1. Synthesis and structure-activity relationships in a new class of 3-, 4- and 5-pyridyl-2(1H)-quinolone derivatives

A series of 3-, 4-, and 5-pyridyl-2(1H)-quinolone derivatives with H or HO or CH3O substituents in the 8-position were prepared and tested for positive inotropic activity. Several derivatives, especially 29, 9b, and 27 with a pyridyl ring in the 5-position, were ca. 2-10 times more potent on left gu...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 29; no. 12; pp. 2427 - 2432
Main Authors:	Leclerc, Gerard, Marciniak, Gilbert, Decker, Nicole, Schwartz, Jean
Format:	Journal Article
Language:	English
Published:	United States American Chemical Society 01-12-1986
Subjects:	Animals Atrial Function Cardiotonic Agents - chemical synthesis Female Guinea Pigs Heart Atria - drug effects In Vitro Techniques Indicators and Reagents Magnetic Resonance Spectroscopy Male Myocardial Contraction - drug effects Pyridines - chemical synthesis Pyridines - pharmacology Quinolines - chemical synthesis Quinolines - pharmacology Structure-Activity Relationship
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Summary:	A series of 3-, 4-, and 5-pyridyl-2(1H)-quinolone derivatives with H or HO or CH3O substituents in the 8-position were prepared and tested for positive inotropic activity. Several derivatives, especially 29, 9b, and 27 with a pyridyl ring in the 5-position, were ca. 2-10 times more potent on left guinea pig atria than sulmazole (ARL-115) and milrinone used as references. Some structure-activity relationships are discussed.
Bibliography:	ark:/67375/TPS-CMPRC8KZ-1 istex:38E659ACF1B786AEB28250F99A2DDADABC030519 ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00162a002