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Bioorg Med Chem Lett. 2009 Nov 1;19(21):6148-56. doi: 10.1016/j.bmcl.2009.09.017. Epub 2009 Sep 10.

Piperazinyl-glutamate-pyrimidines as potent P2Y12 antagonists for inhibition of platelet aggregation.

Author information

1
Department of Medicinal Chemistry, Pfizer Global Research and Development, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. john.j.parlow@pfizer.com

Abstract

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.

PMID:
19796941
DOI:
10.1016/j.bmcl.2009.09.017
[Indexed for MEDLINE]

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