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

…, F Leroux, B Deprez, R Deprez-Poulain

Index: Maingot, Lucie; Elbakali, Jamal; Dumont, Julie; Bosc, Damien; Cousaert, Nicolas; Urban, Agathe; Deglane, Gaelle; Villoutreix, Bruno; Nagase, Hideaki; Sperandio, Olivier; Leroux, Florence; Deprez, Benoit; Deprez-Poulain, Rebecca European Journal of Medicinal Chemistry, 2013 , vol. 69, p. 244 - 261

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Citation Number: 7

Abstract

Abstract 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 ...