期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 10, 页码 3161-3164出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.03.096
关键词
P2X7; P2X7 antagonist; Lead optimisation
High-throughput screening identified compound 1 as a potent P2X(7) receptor antagonist suitable for lead optimisation. Structure-activity relationships (SAR) of a series of (1H-pyrazol-4-yl)acetamides were investigated and compound 32 was identified as a potent P2X(7) antagonist with enhanced potency and favourable physicochemical and pharmacokinetic properties. (C) 2010 Elsevier Ltd. All rights reserved.
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