2-氰基嘧啶：半胱氨酸蛋白酶组织蛋白酶K抑制剂的一种新化学类型。
2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K.
作者信息
Altmann Eva, Aichholz Reiner, Betschart Claudia, Buhl Thomas, Green Jonathan, Irie Osamu, Teno Naoki, Lattmann René, Tintelnot-Blomley Marina, Missbach Martin
机构信息
Novartis Institutes of BioMedical Research, CH-4002 Basel, Switzerland.
出版信息
J Med Chem. 2007 Feb 22;50(4):591-4. doi: 10.1021/jm0613525. Epub 2007 Jan 27.
PMID:17256925
Abstract
Starting from the purine lead structure 1, a new series of cathepsin K inhibitors based on a pyrimidine scaffold have been explored. Investigations of P3 and P2 substituents based on molecular modeling suggestions resulted in potent cathepsin K inhibitors with an improved selectivity profile over other cathepsins.
摘要
从嘌呤先导结构1出发，已探索了一系列基于嘧啶骨架的新型组织蛋白酶K抑制剂。根据分子模拟建议对P3和P2取代基进行研究，得到了对组织蛋白酶K具有强效抑制作用且对其他组织蛋白酶选择性更高的抑制剂。
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