Lizarzaburu, Mike; Turcotte, Simon; Du, Xiaohui; Duquette, Jason; Fu, Angela; Houze, Jonathan; Li, Leping; Liu, Jinqian; Murakoshi, Michiko; Oda, Kozo; Okuyama, Ryo; Nara, Futoshi; Reagan, Jeff; Yu, Ming; Medina, Julio C. published the artcile< Discovery and optimization of a novel series of GPR142 agonists for the treatment of type 2 diabetes mellitus>, Electric Literature of 112-63-0, the main research area is alkylphenylalaninamide pyridinylphenylamine oxobipyridinylamine preparation GPR142 agonist; structure alkylphenylalaninamide pyridinylphenylamine oxobipyridinylamine GPR142 agonism exposure; cytochrome P 450 inhibition alkylphenylalaninamide pyridinylphenylamine oxobipyridinylamine.
N-alkylphenylalaninamides of pyridinylphenyl- and oxobipyridinylamines such as I were prepared as GPR142 agonists for potential use as antidiabetic agents for type 2 diabetes and tested for their agonism of GPR142 in vitro and in human plasma and their inhibition of cytochrome P 450 enzymes such as isoforms 3A4 and 2D6. Optimization of the original lead compound gave agonists 90 times more potent against human GPR142. Inhibition of cytochrome P 450 isoforms 3A4 and 2D6 was reduced by increasing the polarity of the biarylamine moiety. The pharmacokinetics of I and a thiazolylmethyl phenylalaninamide of an aminopyridinylbenzoate were determined in rats.
Bioorganic & Medicinal Chemistry Letters published new progress about G protein-coupled receptors Role: BSU (Biological Study, Unclassified), BIOL (Biological Study) (GPR 142). 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, Electric Literature of 112-63-0.
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