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Bioorg Med Chem Lett. 2008 Oct 15;18(20):5402-5. doi: 10.1016/j.bmcl.2008.09.048. Epub 2008 Sep 14.

2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.

Author information

1
Department of Medicinal Chemistry, Neurocrine Biosciences, 12780 El Camino Real, San Diego, CA 92130, USA. mmoorjani@neurocrine.com

Abstract

In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited excellent potency, selectivity over A(1) and improved solubility of >4 mg/mL at pH 8.0. In addition, compound 35 had good metabolic stability with a scaled intrinsic clearance of 3 mL/min/kg (HLM) and demonstrated efficacy in the haloperidol induced catalepsy model.

PMID:
18835161
DOI:
10.1016/j.bmcl.2008.09.048
[Indexed for MEDLINE]

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