1. Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase.
- Author
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Ruf S, Hallur MS, Anchan NK, Swamy IN, Murugesan KR, Sarkar S, Narasimhulu LK, Putta VPRK, Shaik S, Chandrasekar DV, Mane VS, Kadnur SV, Suresh J, Bhamidipati RK, Singh M, Burri RR, Kristam R, Schreuder H, Czech J, Rudolph C, Marker A, Langer T, Mullangi R, Yura T, Gosu R, Kannt A, Dhakshinamoorthy S, and Rajagopal S
- Subjects
- Dose-Response Relationship, Drug, Enzyme Inhibitors chemical synthesis, Enzyme Inhibitors chemistry, Humans, Molecular Structure, Niacinamide chemical synthesis, Niacinamide chemistry, Nicotinamide N-Methyltransferase metabolism, Structure-Activity Relationship, Enzyme Inhibitors pharmacology, Niacinamide pharmacology, Nicotinamide N-Methyltransferase antagonists & inhibitors
- Abstract
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 ∼80% at 2 h when dosed in mice orally at 50 mg/kg., (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- Published
- 2018
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