基于邻苯二甲酰亚胺的内酰胺和环状脲作为 ROCK2 选择性抑制剂。
Phthalazinone-based lactams and cyclic ureas as ROCK2 selective inhibitors.
机构信息
Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
Research & Early Development, Bristol Myers Squibb, P.O. Box 5400, Princeton, NJ 08543-5400, USA.
出版信息
Bioorg Med Chem Lett. 2023 May 15;88:129304. doi: 10.1016/j.bmcl.2023.129304. Epub 2023 Apr 28.
PMID:37119973
Abstract
Derivatives of lactam, cyclic urea and carbamate were explored as aniline amide replacements in a series of phthalazinone-based ROCK inhibitors. Potent ROCK2 inhibitors such as 22 were identified with excellent overall kinase selectivity as well as good isoform selectivity over ROCK1.
摘要
研究了内酰胺、环脲和氨基甲酸酯的衍生物作为一系列苯并嗪酮基 ROCK 抑制剂中苯胺酰胺的替代品。发现了强效的 ROCK2 抑制剂，如 22，具有优异的整体激酶选择性以及对 ROCK1 的良好亚型选择性。
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