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Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes

[Image: see text] A novel series of pyridones were discovered as potent EP3 antagonists. Optimization guided by EP3 binding and functional assays as well as by eADME and PK profiling led to multiple compounds with good physical properties, excellent oral bioavailability, and a clean in vitro safety...

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Pubblicato in:ACS Med Chem Lett
Autori principali: Zhang, Xuqing, Zhu, Bin, Guo, Lili, Bakaj, Ivona, Rankin, Matthew, Ho, George, Kauffman, Jack, Lee, Seunghun P., Norquay, Lisa, Macielag, Mark J.
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2021
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC7957929/
https://ncbi.nlm.nih.gov/pubmed/33738072
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00667
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