Title of article
2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A2A antagonists with improved solubility and metabolic stability
Author/Authors
Manisha Moorjani، نويسنده , , Zhiyong Luo، نويسنده , , Emily Lin، نويسنده , , Binh G. Vong، نويسنده , , Yongsheng Chen، نويسنده , , Xiaohu Zhang، نويسنده , , Jaimie K. Rueter، نويسنده , , Raymond S. Gross، نويسنده , , Marion C. Lanier، نويسنده , , John E. Tellew، نويسنده , , John P. Williams، نويسنده , , Sandra M. Lechner، نويسنده , , Siobhan Malany، نويسنده , , Mark Santos، نويسنده , , Mar?a I. Crespo، نويسنده , , Jose Luis Diaz-Rossello، نويسنده , , John Saunders، نويسنده , , Deborah H. Slee، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
5402
To page
5405
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 A1 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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
800022
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