2-cyano-pyrimidines: A new chemotype for inhibitors of the cysteine protease cathepsin K
2-cyano-pyrimidines: A new chemotype for inhibitors of the cysteine protease cathepsin K
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DOI：
10.1021/jm0613525
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发表时间：
2007-02-22
影响因子：
7.3
通讯作者：
Missbach, Martin
中科院分区：
文献类型：
--
作者：
Altmann, Eva;Aichholz, Reiner;Missbach, Martin
从嘌呤先导结构1开始，探索了一系列基于嘧啶支架的新型组织蛋白酶K抑制剂。基于分子模型建议对 P3 和 P2 取代基的研究产生了有效的组织蛋白酶 K 抑制剂，与其他组织蛋白酶相比，其选择性得到了改善。
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.