4.5 Article

Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 28, Issue 5, Pages 922-925

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2018.01.058

Keywords

Nicotinamide N-methyltransferase (NNMT); Ncotinamide; Methyl-nicotinamide (MNA); Obesity; Diabetes

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Nicotinamide N-methyltransferase (NNMT) has been linked to obesity and diabetes. We have identified a novel nicotinamide (NA) analog, compound 12 that inhibited NNMT enzymatic activity and reduced the formation of 1-methyl-nicotinamide (MNA), the primary metabolite of NA by similar to 80% at 2 h when dosed in mice orally at 50 mg/kg. (C) 2018 Elsevier Ltd. All rights reserved.

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