Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase

Autor:	Nisha K. Anchan, Thomas Langer, Vishal Subhash Mane, Raghunadha Reddy Burri, Christine Rudolph, Herman Schreuder, Joerg Czech, Ramachandraiah Gosu, Rajendra Kristam, Saravanakumar Dhakshinamoorthy, Ramesh Mullangi, Juluri Suresh, Mahanandeesha S. Hallur, Sridharan Rajagopal, Takeshi Yura, Manvi Singh, Aimo Kannt, Devaraj Venkatapura Chandrasekar, Shama Shaik, Sanjay Venkatachalapathi Kadnur, V.P. Rama Kishore Putta, Lokesh Kananti Narasimhulu, Karthikai Raj Murugesan, Ravi Kanth Bhamidipati, Sven Ruf, Indu N. Swamy, Alexander Marker, Sayantani Sarkar
Rok vydání:	2018
Předmět:	Niacinamide 0301 basic medicine Clinical Biochemistry Pharmaceutical Science Nicotinamide N-methyltransferase Pharmacology Biochemistry Structure-Activity Relationship 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Diabetes mellitus Drug Discovery Nicotinamide N-Methyltransferase medicine Humans Enzyme Inhibitors Molecular Biology chemistry.chemical_classification Dose-Response Relationship Drug Molecular Structure Nicotinamide Organic Chemistry Primary metabolite medicine.disease 030104 developmental biology Enzyme chemistry 030220 oncology & carcinogenesis Molecular Medicine
Zdroj:	Bioorganic & Medicinal Chemistry Letters. 28:922-925
ISSN:	0960-894X
DOI:	10.1016/j.bmcl.2018.01.058
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0692f15941b73b65689828e71e37e26f https://doi.org/10.1016/j.bmcl.2018.01.058 Zobrazit plný text záznamu Full Text from ScienceDirect