期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 20, 页码 5402-5405出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.09.048
关键词
A(2A) antagonists; adenosine receptor; Parkinson's disease
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. (C) 2008 Elsevier Ltd. All rights reserved.
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