New non-hydroxamic ADAMTS-5 inhibitors based on the 1,2,4-triazole-3-thiol scaffold
Lucie Maingot1, Florence Leroux, Valérie Landry
1INSERM U761 Biostructures and Drug Discovery, Univ. Lille Nord de France.
Bioorganic & Medicinal Chemistry Letters
|September 18, 2010
Abstract:
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.
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