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ID: ALA4184280

Journal: Bioorg Med Chem Lett

Title: Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase.

Authors: 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, Rajagopal S.

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.

CiteXplore: 29433927

DOI: 10.1016/j.bmcl.2018.01.058