Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase

被引：29

作者：

Ruf, Sven ^{[1
]}

Hallur, Mahanandeesha Siddappa ^{[2
]}

Anchan, Nisha K. ^{[2
]}

Swamy, Indu N. ^{[2
]}

Murugesan, Karthikai Raj ^{[2
]}

Sarkar, Sayantani ^{[2
]}

Narasimhulu, Lokesh Kananti ^{[2
]}

Putta, V. P. Rama Kishore ^{[2
]}

Shaik, Shama ^{[3
,4
]}

Chandrasekar, Devaraj Venkatapura ^{[5
]}

Mane, Vishal Subhash ^{[3
,4
]}

Kadnur, Sanjay Venkatachalapathi ^{[3
,4
]}

Suresh, Juluri ^{[3
,4
]}

Bhamidipati, Ravi Kanth ^{[5
]}

Singh, Manvi ^{[6
]}

Burri, Raghunadha Reddy ^{[6
]}

Kristam, Rajendra ^{[6
]}

Schreuder, Herman ^{[1
]}

Czech, Joerg ^{[1
]}

Rudolph, Christine ^{[1
]}

Marker, Alexander ^{[7
]}

Langer, Thomas ^{[8
]}

Mullangi, Ramesh ^{[5
]}

Yura, Takeshi ^{[2
]}

Gosu, Ramachandraiah ^{[5
]}

Kannt, Aimo ^{[9
,10
]}

Dhakshinamoorthy, Saravanakumar ^{[3
,4
]}

Rajagopal, Sridharan ^{[2
]}

机构：

[1] Sanofi Aventis Deutschland GmbH, Integrated Drug Discovery, D-65926 Frankfurt, Germany

[2] Jubilant Biosys Ltd, Dept Med Chem, Bangalore 560022, Karnataka, India

[3] Jubilant Biosys Ltd, Dept Discovery Biol, Bangalore 560022, Karnataka, India

[4] Jubilant Biosys Ltd, Dept Drug Metab & Pharmacokinet, Bangalore 560022, Karnataka, India

[5] Jubilant Biosys Ltd, Dept Biol Struct, Bangalore 560022, Karnataka, India

[6] Jubilant Biosys Ltd, Dept Computat Chem, Bangalore 560022, Karnataka, India

[7] Sanofi Aventis Deutschland GmbH, R&D Drug Metab & Pharmacokinet, D-65926 Frankfurt, Germany

[8] Sanofi Aventis Deutschland GmbH, Biol Res, D-65926 Frankfurt, Germany

[9] Sanofi Aventis Deutschland GmbH, R&D Diabet, D-65926 Frankfurt, Germany

[10] Heidelberg Univ, Med Fac Mannheim, Inst Expt Pharmacol, D-68167 Mannheim, Germany

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2018年 / 28卷 / 05期

关键词：

Nicotinamide N-methyltransferase (NNMT); Ncotinamide; Methyl-nicotinamide (MNA); Obesity; Diabetes; CELL CARCINOMA; ADIPOSE-TISSUE; TUMOR-MARKER; EXPRESSION; IDENTIFICATION; PRODUCT; OBESITY; MOUSE; ASSAY; RAT;

D O I：

10.1016/j.bmcl.2018.01.058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 similar to 80% at 2 h when dosed in mice orally at 50 mg/kg. (C) 2018 Elsevier Ltd. All rights reserved.

引用

页码：922 / 925

页数：4

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