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Novel N-substituted 2-phenyl-1-sulfonylamino-cyclopropane carboxylates as selective ADAMTS-5 (Aggrecanase-2) inhibitors |
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| Authors: | Makoto Shiozaki Katsuya Maeda Tomoya Miura 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 |
| Affiliation: | 1. Central Pharmaceutical Research Institute, Japan Tobacco Inc., 1-1, Murasaki-cho, Takatsuki, Osaka 569-1125, Japan;2. Array BioPharma Inc., 3200 Walnut Street, Boulder, CO 80301, USA |
| Abstract: | 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 IC50 < 0.1 μM with excellent selectivity over MMP-1 and TACE. |
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