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© Research
Publication : European journal of medicinal chemistry

Aggrecanase-2 inhibitors based on the acylthiosemicarbazide zinc-binding group

Scientific Fields
Diseases
Organisms
Applications
Technique

Published in European journal of medicinal chemistry - 30 Aug 2013

Maingot L, Elbakali J, Dumont J, Bosc D, Cousaert N, Urban A, Deglane G, Villoutreix B, Nagase H, Sperandio O, Leroux F, Deprez B, Deprez-Poulain R

Link to Pubmed [PMID] – 24044937

Eur J Med Chem 2013 Nov;69:244-61

Osteoarthritis is a disabling disease characterized by the articular cartilage breakdown. Aggrecanases are potential therapeutic targets for the treatment of this pathology. At the starting point of this project, an acylthiosemicarbazide was discovered to inhibit aggrecanase-2. The acylthiosemicarbazide Zn binding group is also a convenient linker for library synthesis. A focused library of 920 analogs was thus prepared and screened to establish structure-activity relationships. The modification of the acylthiosemicarbazide was also explored. This strategy combining library design and discrete compounds synthesis yielded inhibitor 35, that is highly selective for aggrecanases over a panel of metalloproteases and inhibits the degradation of native fully glycosylated aggrecan. A docking study generated binding conformations explaining the structure-activity relationships.

https://www.ncbi.nlm.nih.gov/pubmed/24044937