Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors
Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors
复制标题
DOI：
10.1016/j.bmcl.2009.08.093
复制
发表时间：
2009-11-01
影响因子：
2.7
通讯作者：
Inaba, Takashi
中科院分区：
文献类型：
--
作者：
Shiozaki, Makoto;Imai, Hiroto;Inaba, Takashi
合成了一系列1-磺酰基氨基环丙基羧酸盐作为agrecanase -2 （ADAMTS-5）抑制剂。经过对中心环丙烷核心的绝对立体化学和取代基的深入研究，我们发现化合物22具有Agg-2 IC(50) = 7.4 nM，是迄今为止报道的最有效的ADAMTS-5抑制剂。(c) 2009 Elsevier Ltd.版权所有。
A series of 1-sulfonylaminocyclopropanecarboxylates was synthesized as ADAMTS-5 (Aggrecanase-2) inhibitors. After an intensive investigation of the central cyclopropane core including its absolute stereochemistry and substituents, we found compound 22 with an Agg-2 IC(50) = 7.4 nM, the most potent ADAMTS-5 inhibitor reported so far. (c) 2009 Elsevier Ltd. All rights reserved.