新型N-取代的2-苯基-1-磺酰氨基环丙烷羧酸盐作为选择性ADAMTS-5（软骨聚集蛋白聚糖酶-2）抑制剂。
Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors.
作者信息
Shiozaki Makoto, Maeda Katsuya, Miura Tomoya, Ogoshi Yosuke, Haas Julia, Fryer Andrew M, Laird Ellen R, Littmann Nicole M, Andrews Steven W, Josey John A, Mimura Takayuki, Shinozaki Yuichi, Yoshiuchi Hiromi, Inaba Takashi
机构信息
Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan.
出版信息
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1575-80. doi: 10.1016/j.bmcl.2009.02.024. Epub 2009 Feb 11.
A series of N-substituted sulfonylamino-alkanecarboxylate ADAMTS-5 (Aggrecanase-2) inhibitors has been synthesized and the in vitro enzyme SAR is discussed. This report is the first example of carboxylate-based ADAMTS-5 inhibitors which show strong potency of IC(50)<0.1muM with excellent selectivity over MMP-1 and TACE.
已经合成了一系列N-取代的磺酰氨基链烷羧酸酯ADAMTS-5（软骨聚集蛋白聚糖酶-2）抑制剂，并讨论了其体外酶活性的构效关系。本报告是基于羧酸酯的ADAMTS-5抑制剂的首个实例，这些抑制剂显示出强大的效力，IC(50)<0.1μM，对MMP-1和肿瘤坏死因子α转换酶具有优异的选择性。
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