Cardiotonic agents. 1. Synthesis and structure-activity relationships in a new class of 3-, 4- and 5-pyridyl-2(1H)-quinolone derivatives
作者:Gerard Leclerc、Gilbert Marciniak、Nicole Decker、Jean Schwartz
DOI:10.1021/jm00162a002
日期:1986.12
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
制备了一系列在8位具有H或HO或CH3O取代基的3-,4-和5-吡啶基-2(1H)-喹诺酮衍生物,并测试了其正性肌力活性。大约有几个衍生物,特别是在5位带有吡啶环的29、9b和27。左豚鼠心房的效力是舒马唑(ARL-115)和米力农用作参考的2-10倍。讨论了一些构效关系。