Buckman B O, Mohan R, Koovakkat S, Liang A, Trinh L, Morrissey M M
Berlex Biosciences, Richmond, CA 94804, USA.
Bioorg Med Chem Lett. 1998 Aug 18;8(16):2235-40. doi: 10.1016/s0960-894x(98)00386-2.
The synthesis of amidinoaryloxy 9-benzyl-8-methyl-9H-purine, 7,8-dihydropteridine-6(5H)-one and 5,7-dihydropyrimido[4,5-b][1,4]oxazine-6-one inhibitors of Factor Xa is described. These compounds show nanomolar potency against FXa and maintain high selectivity over thrombin and trypsin.
描述了氨脒基芳氧基9-苄基-8-甲基-9H-嘌呤、7,8-二氢蝶啶-6(5H)-酮和5,7-二氢嘧啶并[4,5-b][1,4]恶嗪-6-酮Xa因子抑制剂的合成。这些化合物对Xa因子显示出纳摩尔级别的效力，并且对凝血酶和胰蛋白酶保持高选择性。
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