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In this Letter we describe the design, synthesis, screening, and optimization of a new family of ADAMTS-5 inhibitors. These inhibitors display an original 1,2,4-triazole-3-thiol scaffold as a putative zinc binding-group. In vitro results are rationalized by in silico docking of the compounds in ADAMTS-5's crystal structure.

Original publication

DOI

10.1016/j.bmcl.2010.08.108

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/11/2010

Volume

20

Pages

6213 - 6216

Keywords

ADAM Proteins, ADAMTS5 Protein, Binding Sites, Computer Simulation, Drug Evaluation, Preclinical, Humans, Indicators and Reagents, Models, Molecular, Osteoarthritis, Protease Inhibitors, Protein Binding, Protein Conformation, Structure-Activity Relationship, Triazoles, X-Ray Diffraction