基于氨基双环芳基的口服生物可利用凝血酶抑制剂的设计、合成与测试。
Design, synthesis and testing of amino-bicycloaryl based orally bioavailable thrombin inhibitors.
作者信息
Rewinkel J B, Lucas H, Smit M J, Noach A B, van Dinther T G, Rood A M, Jenneboer A J, van Boeckel C A
机构信息
NV Organon, Research and Development, Oss, The Netherlands.
出版信息
Bioorg Med Chem Lett. 1999 Oct 4;9(19):2837-42. doi: 10.1016/s0960-894x(99)00483-7.
Abstract
Replacement of the highly basic benzamidine moiety with moderate basic amino-bicycloaryl moieties in a series of thrombin inhibitors related to NAPAMP provided potent enzyme inhibition and significant improvements in membrane transport and oral bioavailability.
摘要
在一系列与NAPAMP相关的凝血酶抑制剂中，用中等碱性的氨基双环芳基部分取代高碱性的苯甲脒部分，可提供有效的酶抑制作用，并显著改善膜转运和口服生物利用度。
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