期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 21, 期 12, 页码 3632-3636出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.04.097
关键词
S1P(4) receptor antagonists; S1P(1-3,5) receptor family; 5-Aryl furan-2-arylcarboxamide
资金
- National Institute of Health Molecular Library Screen Center Network [U54 MH084512A]
Selective S1P(4) receptor antagonists could be novel therapeutic agents for the treatment of influenza infection in addition to serving as a useful tool for understanding S1P(4) receptor biological functions. 5-(2,5-Dichlorophenyl)-N-(2,6-dimethylphenyl)furan-2-carboxamide was identified from screening the Molecular Libraries-Small Molecule Repository (MLSMR) collection and selected as a promising S1P(4) antagonist hit with moderate in vitro potency and high selectivity against the other family receptor subtypes (S1P(1-3,5)). Rational chemical modifications of the hit allowed the disclosure of the first reported highly selective S1P(4) antagonists with low nanomolar activity and adequate physicochemical properties suitable for further lead-optimization studies. (C) 2011 Elsevier Ltd. All rights reserved.
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