Development and characterization of 3-(benzylsulfonamido) benzamides as potent and selective SIRT2 inhibitors

…, L Quinti, H Wang, SH Choi, AG Kazantsev…

Index: Khanfar, Mohammad A.; Quinti, Luisa; Wang, Hua; Choi, Soo Hyuk; Kazantsev, Aleksey G.; Silverman, Richard B. European Journal of Medicinal Chemistry, 2014 , vol. 76, p. 414 - 426

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Citation Number: 12

Abstract

Abstract Inhibitors of sirtuin-2 deacetylase (SIRT2) have been shown to be protective in various models of Huntington's disease (HD) by decreasing polyglutamine aggregation, a hallmark of HD pathology. The present study was directed at optimizing the potency of SIRT2 inhibitors containing the neuroprotective sulfobenzoic acid scaffold and improving their pharmacology. To achieve that goal, 176 analogues were designed, synthesized, ...