| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372902 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
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,