Casimiro-Garcia, Agustin; Allais, Christophe; Brennan, Agnes; Choi, Chulho; Dower, Gabriela; Farley, Kathleen A.; Fleming, Margaret; Flick, Andrew; Frisbie, Richard K.; Hall, Justin; Hepworth, David; Jones, Hannah; Knafels, John D.; Kortum, Steve; Lovering, Frank E.; Mathias, John P.; Mohan, Sashi; Morgan, Paul M.; Parng, Chuenlei; Parris, Kevin; Pullen, Nick; Schlerman, Franklin; Stansfield, John; Strohbach, Joseph W.; Vajdos, Felix F.; Vincent, Fabien; Wang, Hong; Wang, Xiaolun; Webster, Robert; Wright, Stephen W. published the artcile< Discovery of a Series of Pyrimidine Carboxamides as Inhibitors of Vanin-1>, Recommanded Product: Ethyl 2-chloropyrimidine-5-carboxylate, the main research area is pyrimidine carboxamide vanin inhibitor pharmacokinetic ADME.
A diaryl ketone series was identified as vanin-1 inhibitors from a high-throughput screening campaign. While this novel scaffold provided valuable probe 2 that was used to build target confidence, concerns over the ketone moiety led to the replacement of this group. The successful replacement of this moiety was achieved with pyrimidine carboxamides derived from cyclic secondary amines that were extensively characterized using biophys. and crystallog. methods as competitive inhibitors of vanin-1. Through optimization of potency and physicochem. and ADME properties, and guided by co-crystal structures with vanin-1, 3 was identified with a suitable profile for advancement into preclin. development.
Journal of Medicinal Chemistry published new progress about Crystal structure. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, Recommanded Product: Ethyl 2-chloropyrimidine-5-carboxylate.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia