期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 19, 期 1, 页码 642-649出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.10.038
关键词
PDE10A inhibition; Phenylimidazole-pyrazolo; [1,5-c]quinazolines; Structure-activity relationships
A series of phenylimidazole-pyrazolo[1,5-c]quinazolines 1a-q was designed, synthesized and characterised as a novel class of potent phophodiesterase 10A (PDE10A) inhibitors. In this series, 2,9-dimethyl-5-(2-(1-methyl-4-phenyl-1H-imidazol-2-yl)ethyl)pyrazolo[1,5-c]quinazoline (1q) showed the highest affinity for PDE10A enzyme (IC50 = 16 nM). (C) 2010 Elsevier Ltd. All rights reserved.
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