Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1372888 | Bioorganic & Medicinal Chemistry Letters | 2009 | 9 Pages |
Piperazinyl-glutamate-pyrimidines were prepared with oxygen, nitrogen, and sulfur substitution at the 4-position of the pyrimidine leading to highly potent P2Y12 antagonists. In particular, 4-substituted piperidine-4-pyrimidines provided compounds with exceptional potency. Pharmacokinetic and physicochemical properties were fine-tuned through modifications at the 4-position of the piperidine ring leading to compounds with good human PRP potency, selectivity, clearance and oral bioavailability.
Graphical abstractPiperazinyl-glutamate-pyrimidines were prepared with oxygen, nitrogen, and sulfur substitution at the 4-position (R4) of the pyrimidine leading to highly potent P2Y12 antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide