期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 13, 页码 3471-3475出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.05.010
关键词
CB1 receptor; Rimonabant; Hit-to-lead; SAR; Pyrrolo[1,2-a]quinoxaline
Hit-to-lead optimization of a novel series of N-alkyl-N-[2-oxo-2-(4-aryl-4H-pyrrolo[1,2-a]quinoxaline-5yl)-ethyl]-carboxylic acid amides, derived from a high throughput screening (HTS) hit, are described. Subsequent optimization led to identification of in vitro potent cannabinoid 1 receptor (CB1R) antagonists representing a new class of compounds in this area. (C) 2009 Elsevier Ltd. All rights reserved.
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