Document Report Card

ID: ALA1126735

Journal: J Med Chem

Title: Synthesis and biological evaluation of antiplatelet 2-aminochromones.

Authors: Morris J, Wishka DG, Lin AH, Humphrey WR, Wiltse AL, Gammill RB, Judge TM, Bisaha SN, Olds NL, Jacob CS.

Abstract: The synthesis and biological evaluation of a series of antiplatelet 2-morpholinylchromones has been described. Modification of the C-7 phenylmethoxy group of 8-methyl-7-(phenylmethoxy)-2-(4-morpholinyl)-4H-1-benzopyran-4-one (2) has led to the discovery of a series of 7-[(amino-ethyl)oxy]-8-methyl derivatives which are potent inhibitors of ADP-induced platelet aggregation. Several members of this class proved active in preventing platelet-dependent thrombus formation in the dog, including 8-methyl-7-[2-(4-methyl-1-piperazinyl)ethoxy]-2-(4- morpholinyl)-4H-1-benzopyran-4-one (39) which was devoid of hemodynamic effects at the effective antithrombotic dose.

CiteXplore: 8336341

DOI: 10.1021/jm00066a012