Selective Human Sirtuin-2 Inhibitors, the Therapeutic Candidate for Huntington's Disease

NU 2012-145

Inventors

Richard Silverman*

Hua Wang

Mohammad Khanfar

Aleksey Kazantsev

Short Description

Selective human sirtuin-2 inhibitors for use in treating Huntington's disease

Abstract

Northwestern researchers have discovered a new series of selective human sirtuin-2 inhibitors which show excellent neuronal protection in the Huntington's disease model. Human sirtuin-2 is a therapeutic target of numerous age-related neuronal degenerative diseases, including Huntington's disease, Parkinson's disease, and Alzheimer's disease. These new compounds were developed using pharmacophere exploration and SAR analysis of a lead compound. This group exhibits improved potency, selectivity and bioavailability and thus are expected to exhibit a promising pharmacological profile. 

Applications

• Treatment of neurodegenerative diseases, such as Huntington's disease, Parkinson's disease and Alzheimer's disease

Advantages

• More potent and selective than previous human sirtuin-2 inhibitors
• Improved pharmaceutical properties and promising drug candidate

Publication

Choi S, Quinti L, Kazantsev A and Silverman R (2012) 3-(N-Arylsulfamoyl)benzamides, inhibitors of human sirtuin type 2 (SIRT2). Bioorganic & Medicinal Chemistry Letters. 22: 2789-2793.

IP Status

Issued US Patent Nos. 9,371,277; 9,533,947 and 9,890,117