13575-40-1Relevant academic research and scientific papers
Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
Ruf, Sven,Hallur, Mahanandeesha Siddappa,Anchan, Nisha K.,Swamy, Indu N.,Murugesan, Karthikai Raj,Sarkar, Sayantani,Narasimhulu, Lokesh Kananti,Putta, V.P. Rama Kishore,Shaik, Shama,Chandrasekar, Devaraj Venkatapura,Mane, Vishal Subhash,Kadnur, Sanjay Venkatachalapathi,Suresh, Juluri,Bhamidipati, Ravi Kanth,Singh, Manvi,Burri, Raghunadha Reddy,Kristam, Rajendra,Schreuder, Herman,Czech, Joerg,Rudolph, Christine,Marker, Alexander,Langer, Thomas,Mullangi, Ramesh,Yura, Takeshi,Gosu, Ramachandraiah,Kannt, Aimo,Dhakshinamoorthy, Saravanakumar,Rajagopal, Sridharan
, p. 922 - 925 (2018)
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.
Substituted Aminopyridines as Fluorescent Reporters for Amide Hydrolases
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, (2010/07/04)
The present invention provides conjugates comprising a substituted aminopyridine covalently attached to an organic molecule via an amide bond. Such conjugates find utility as substrates for amide hydrolases, where the substituted aminopyridine acts as a fluorescent reporter of amide hydrolase activity. As a result, the conjugates described herein can advantageously be used in assays to detect amide hydrolase activity based upon measuring the fluorescence of a substituted aminopyridine that is released after amide hydrolysis. The conjugates of the present invention are also particularly useful in screening assays, which enable the identification of inhibitory molecules for amide hydrolases and other enzymes. The identified amide hydrolase inhibitors can be used in the treatment of a variety of diseases and disorders associated with aberrant amide hydrolase activity.
Identification of a urea bioisostere of a triazole oxytocin antagonist
Brown, Alan,Ellis, Dave,Wallace, Olga,Ralph, Michael
scheme or table, p. 1851 - 1853 (2010/07/06)
A series of azetidine ureas were investigated as potential bioisosteres of previously reported azetidinyltriazole oxytocin antagonists. Although potency was somewhat reduced in several close-in analogues, one compound, 9, was both a potent oxytocin antagonist and demonstrated significant selectivity over the closely related vasopressin V1A receptor.
