Cookies on this website
We use cookies to ensure that we give you the best experience on our website. If you click 'Continue' we'll assume that you are happy to receive all cookies and you won't see this message again. Click 'Find out more' for information on how to change your cookie settings.

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

Bioorganic & medicinal chemistry letters

Publication Date

11/2010

Volume

20

Pages

6213 - 6216

Addresses

INSERM U761 Biostructures and Drug Discovery, Univ. Lille Nord de France.

Keywords

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