Inhibitors of blood platelet cAMP phosphodiesterase. 4. Structural variation of the side-chain terminus of water-soluble 1, 3-dihydro-2H-imidazo [4, 5-b] quinolin-2-one …

NA Meanwell, P Hewawasam, JA Thomas…

Index: Meanwell, Nicholas A.; Hewawasam, Piyasena A.; Thomas, Jeanine; Wright, J. J. Kim; Russell, John W.; et al. Journal of Medicinal Chemistry, 1993 , vol. 36, # 22 p. 3251 - 3264

Full Text: HTML

Citation Number: 14

Abstract

1-(Cyclohexylmethy1)-4-[4-[(2, 3-dihydro-2-0~ 0-lH-imidaz0 [4, 5-b] quinolin-7-yl) oxyl-l- oxobutyllpiperazine (2) was previously identified as a potent, water-soluble inhibitor of human blood platelet cAMP phosphodiesterase and of induced aggregation in vitro that demonstrated effective antithrombotic activity in animal models of thrombosis. Although 2 exhibited 25% oral bioavailability in rats, pharmacokinetic studies conducted in monkeys ...