1-氨基异喹啉作为脒的生物电子等排体用于口服活性凝血酶抑制剂的设计与合成。
1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors.
作者信息
Rewinkel J B, Lucas H, van Galen P J, Noach A B, van Dinther T G, Rood A M, Jenneboer A J, van Boeckel C A
机构信息
NV Organon, Scientific Development Group, Oss, The Netherlands.
出版信息
Bioorg Med Chem Lett. 1999 Mar 8;9(5):685-90. doi: 10.1016/s0960-894x(99)00069-4.
Abstract
Replacement of the highly basic benzamidine moiety of NAPAP by the moderately basic 1-aminoisoquinoline moiety resulted in thrombin inhibitors with improved selectivity towards trypsin and enhanced Caco-2 cell permeability.
摘要
将 NAPAP 的高碱性苯甲脒部分替换为中等碱性的 1-氨基异喹啉部分，得到了对胰蛋白酶具有更高选择性且 Caco-2 细胞通透性增强的凝血酶抑制剂。
Zotero 插件