66416-49-7Relevant academic research and scientific papers
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1
Westaway, Susan M.,Thompson, Mervyn,Rami, Harshad K.,Stemp, Geoffrey,Trouw, Leontine S.,Mitchell, Darren J.,Seal, Jon T.,Medhurst, Stephen J.,Lappin, Sarah C.,Biggs, James,Wright, James,Arpino, Sandra,Jerman, Jeffrey C.,Cryan, Jennifer E.,Holland, Vicky,Winborn, Kim Y.,Coleman, Tanya,Stevens, Alexander J.,Davis, John B.,Gunthorpe, Martin J.
scheme or table, p. 5609 - 5613 (2009/06/18)
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the discovery of 6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide (32; SB-782443) which possesses an excellent overall profile and has been progressed into pre-clinical development.
Annelation reactions of enaminones with ethyl acetoacetate. Studies on the β-carbonyl compounds connected with β-polyketides. XI
Takeuchi,Handa,Koyama,Kamata,Goto,Tobinaga
, p. 1655 - 1658 (2007/10/02)
Though condensation at either the carbonyl oxygen or the unsaturated carbon adjacent to nitrogen of enaminones can occur in the reaction with the active methylene of ethyl acetoacetate, the results obtained in the condensation reactions of the enaminones
