Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists

[Image: see text] The identification of highly potent and orally bioavailable GPR39 agonists is reported. Compound 1, found in a phenotypic screening campaign, was transformed into compound 2 with good activity on both the rat and human GPR39 receptor. This compound was further optimized to improve...

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Hauptverfasser: Peukert, Stefan, Hughes, Richard, Nunez, Jill, He, Guo, Yan, Zhao, Jain, Rishi, Llamas, Luis, Luchansky, Sarah, Carlson, Adam, Liang, Guiqing, Kunjathoor, Vidya, Pietropaolo, Mike, Shapiro, Jeffrey, Castellana, Anja, Wu, Xiaoping, Bose, Avirup
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2014
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4190643/
https://ncbi.nlm.nih.gov/pubmed/25313322
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml500240d
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