2 (1H)-Quinolinones with cardiac stimulant activity. 1. Synthesis and biological activities of (six-membered heteroaryl)-substituted derivatives

…, CG Henderson, DA Roberts, KS Ruddock…

Index: Alabaster; Bell; Campbell; Ellis; Henderson; Roberts; Ruddock; Samuels; Stefaniak Journal of Medicinal Chemistry, 1988 , vol. 31, # 10 p. 2048 - 2056

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Citation Number: 48

Abstract

A series of (six-membered heteroary1)-substituted 2 (1H)-quinolinones (1) was synthesized, and structure-activity relationships for cardiac stimulant activity were determined. Most compounds were prepared by acidic hydrolysis of a heteroaryl-2-methoxyquinoline obtained by palladium-catalyzed cross-coupling methodology. Direct reaction of a ppidinylzinc reagent with a 6-haloquinolinone also proved successful. In anesthetized dogs, 6-pyridin- ...