Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carb...

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Synthesis and SAR of 2-phenyl-1-sulfonylaminocyclopropane carboxylates as ADAMTS-5 (Aggrecanase-2) inhibitors.
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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 IC(50)=7.4 nM, the most potent ADAMTS-5 inhibitor reported so far.
Shiozaki M, Imai H, Maeda K, Miura T, Yasue K, Suma A, Yokota M, Ogoshi Y, Haas J, Fryer AM, Laird ER, Littmann NM, Andrews SW, Josey JA, Mimura T, Shinozaki Y, 
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Bioorganic & medicinal chemistry letters 19(21):6213-7, 2009 Nov 1 - Who cited this? | PubMed ID: 19767207 | Fulltext
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