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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6213-7. doi: 10.1016/j.bmcl.2009.08.093. Epub 2009 Sep 3.

Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors.

Author information

1
Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan. makoto.shiozaki@ims.jti.co.jp

Abstract

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 IC50=7.4 nM, the most potent ADAMTS-5 inhibitor reported so far.

PMID:
19767207
DOI:
10.1016/j.bmcl.2009.08.093
[Indexed for MEDLINE]

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