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Discovery of Bicyclic Pyrazoles As Class III Histone Deacetylase SIRT1 and SIRT2 Inhibitors

Eric Therrien,Guillaume Larouche,Natalie Nguyen,Jubrail Rahil,Anne-Marie Lemieux,Zuomei Li,Marielle Fournel,Theresa P. Yan,Anne-Julie Landry,Sylvain Lefebvre,James J. Wang,Kyle MacBeth,Carla Heise,Aaron Nguyen,Jeffrey M. Besterman,Robert Deziel,Amal Wahhab

Bioorganic & medicinal chemistry letters（2015）

Cited 26|Views22
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Abstract
A series of bicyclic pyrazole carboxamides was synthesized and tested for inhibitory activity against the class III deacetylase sirtuin enzymes. Moderate to low micromolar inhibitory activities were obtained against SIRT1 and SIRT2. These bicyclic pyrazole compounds represent a new class of sirtuin inhibitors with a preference for SIRT1 over SIRT2.
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Key words
Sirtuin,SIRT,Inhibitor,Pyrazole,Docking
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