☆ 4.5 Article

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

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS (2009)

期刊

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷 19, 期 21, 页码 6213-6217

出版社

PERGAMON-ELSEVIER SCIENCE LTD

DOI: 10.1016/j.bmcl.2009.08.093

关键词

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

类别

Chemistry, Medicinal Chemistry, Organic

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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 IC(50) = 7.4 nM, the most potent ADAMTS-5 inhibitor reported so far. (c) 2009 Elsevier Ltd. All rights reserved.

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