1160271-23-7Relevant academic research and scientific papers
The identification of 4,7-disubstituted naphthoic acid derivatives as UDP-competitive antagonists of P2Y14
Gauthier, Jacques Yves,Belley, Michel,Deschênes, Denis,Fournier, Jean-Fran?ois,Gagné, Sébastien,Gareau, Yves,Hamel, Martine,Hénault, Martin,Hyjazie, Huda,Kargman, Stacia,Lavallée, Geneviève,Levesque, Jean-Fran?ois,Li, Lianhai,Mamane, Ya?l,Mancini, Joseph,Morin, Nicolas,Mulrooney, Erin,Robichaud, Jo?l,Thérien, Michel,Tranmer, Geoffrey,Wang, Zhaoyin,Wu, Jin,Black, W. Cameron
, p. 2836 - 2839 (2011)
A weak, UDP-competitive antagonist of the pyrimidinergic receptor P2RY 14 with a naphthoic acid core was identified through high-throughput screening. Optimization provided compounds with improved potency but poor pharmacokinetics. Acylglucuronidation was determined to be the major route of metabolism. Increasing the electron-withdrawing nature of the substituents markedly reduced glucuronidation and improved the pharmacokinetic profile. Additional optimization led to the identification of compound 38 which is an 8 nM UDP-competitive antagonist of P2Y14 with a good pharmacokinetic profile.
SUBSTITUTED 2-NAPHTHOIC ACIDS AS ANTAGONISTS OF GPR105 ACTIVITY
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Page/Page column 37; 41; 72, (2009/07/17)
Substituted 2-naphthoic acids of structural formula I are effective as antagonists of the biological activity of GPR105 protein. They are useful for the treatment, control or prevention of disorders responsive to antagonism of this receptor, such as diabe
