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Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2018 Mar 01; Vol. 28 (5), pp. 922-925. Date of Electronic Publication: 2018 Jan 31. - Publication Year :
- 2018
-
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.<br /> (Copyright © 2018 Elsevier Ltd. All rights reserved.)
- 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
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 28
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 29433927
- Full Text :
- https://doi.org/10.1016/j.bmcl.2018.01.058