Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
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 2h when dosed in...
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| Main Authors: | , |
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| Format: | Article (Journal) |
| Language: | English |
| Published: |
1 March 2018
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| In: |
Bioorganic & medicinal chemistry letters
Year: 2018, Volume: 28, Issue: 5, Pages: 922-925 |
| ISSN: | 1464-3405 |
| DOI: | 10.1016/j.bmcl.2018.01.058 |
| Online Access: | Verlag, lizenzpflichtig, Volltext: https://doi.org/10.1016/j.bmcl.2018.01.058 Verlag, lizenzpflichtig, Volltext: http://www.sciencedirect.com/science/article/pii/S0960894X18300696 
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| Author Notes: | Sven Ruf, Mahanandeesha Siddappa Hallur, Nisha K. Anchan, Indu N. Swamy, Karthikai Raj Murugesan, Sayantani Sarkar, Lokesh Kananti Narasimhulu, V. P. Rama Kishore Putta, Shama Shaik, Devaraj Venkatapura Chandrasekar, Vishal Subhash Mane, Sanjay Venkatachalapathi Kadnur, Juluri Suresh, Ravi Kanth Bhamidipati, Manvi Singh, Raghunadha Reddy Burri, Rajendra Kristam, Herman Schreuder, Joerg Czech, Christine Rudolph, Alexander Marker, Thomas Langer, Ramesh Mullangi, Takeshi Yura, Ramachandraiah Gosu, Aimo Kannt, Saravanakumar Dhakshinamoorthy, Sridharan Rajagopal |
| Summary: | 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 2h when dosed in mice orally at 50mg/kg. |
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| Item Description: | Gesehen am 22.07.2020 |
| Physical Description: | Online Resource |
| ISSN: | 1464-3405 |
| DOI: | 10.1016/j.bmcl.2018.01.058 |