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

Makoto Shiozaki,Hiroto Imai,Katsuya Maeda,Tomoya Miura,Katsutaka Yasue,Akira Suma,Masahiro Yokota,Yosuke Ogoshi,Julia Haas,Andrew M Fryer,Ellen R Laird,Nicole M Littmann,Steven W Andrews,John A Josey,Takayuki Mimura,Yuichi Shinozaki,Hiromi Yoshiuchi,Takashi Inaba

Bioorganic & Medicinal Chemistry Letters（2009）

引用 21|浏览21

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摘要

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.

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关键词

SAR,ADAMTS-5 (Aggrecanase-2) inhibitors,2-Phenyl-1-sulfonylaminocyclopropanecarboxylates

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