- Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
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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.
- 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
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supporting information
p. 922 - 925
(2018/02/14)
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- Modification of Pyridine-3-carboxamide (Nicotinamide) by Radical Substitution
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Pyridine-3-carboxamide (1) was reacted with alkyl radicals to give mono-, di-, and tri-alkylated products.The t-butyl radical gives only 6-t-butylpyridine-3-carboxamide (4a).The reactivity decreases in the order of t-butyl, isopropyl, and ethyl radicals.The product 4a reacts further with the 2-phthalimidoethyl radical to give 2- and 4-substituted products 9 and 10, which were transformed into tetrahydronaphthyridinone derivatives 11 and 12.
- Tada, Masaru,Yokoi, Yurie
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- Photochemical Alkylation, Hydroxyalkylation, and Alkoxylation of Pyridinecarboxamides in Alcohol
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The UV-irradiation of 2- and 4-pyridinecarboxamides in alcohol brings about alkylation and/or hydroxyalkylation in the pyridine ring.In the irradiation of 3-pyridinecarboxamide in the presence of sulfuric acid, ionic reaction (alkoxylation at the 2- and 6-position) and radical reaction (alkylation at the 4- and 6-position) occur in parallel.The effects of quenchers indicate that two alkylation products originate from one excited triplet state which is quenched by energy-transfer mechanism and that two alkoxylation products originate from the excited singlet state.
- Sugimori, Akira,Itoh, Hiroshi,Kanai, Mitsuharu,Itoh, Nobuko,Sugiyama, Toru
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p. 2837 - 2846
(2007/10/02)
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- Radiation-induced Alkylation, Hydroxyalkylation, and Reduction of Pyridinecarboxamides in Acidic Alcoholic Solutions
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The γ-irradiation of pyridinecarboxamides in acidic methanol or ethanol brings about substitution of the ring hydrogen by alkyl or hydroxyalkyl groups derived from the solvent alcohols in relatively high G-values.In 2-propanol, little alkylation and hydroxyalkylation occur and reduction of CONH2 to CH2OH occurs in low G-values.
- Sugimori, Akira,Nishijima, Masayuki,Itoh, Hiroshi
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p. 3055 - 3056
(2007/10/02)
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