期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 101, 期 -, 页码 185-204出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.06.041
关键词
A(1) adenosine receptor; Allosteric modulator; G protein-coupled receptors; Anti-nociceptive effect
The 2-amino-3-(p-chlorobenzoyl)thiophene scaffold has been widely employed as a pharmacophore for the identification of small molecules acting as allosteric modulators at the adenosine A(1) receptor. A new series of 2-amino-3-(p-chlorobenzoyl)-4-benzy1-5-arylthiophene derivatives, characterized by the absence as well as the presence of electron-releasing or electron-withdrawing groups on the phenyl ring at the 4- and 5-positions of the thiophene ring, were identified as positive allosteric enhancers at the adenosine A1 receptor in binding (saturation, competition and dissociation kinetics) and functional assays. To better understand the positional requirements of substituents on the 2-amino-3-(p-chlorobenzoyl)thiophene core, the corresponding regioisomeric 4-aryl-5-benzylthiophene analogues were synthesized and found to possess reduced allosteric enhancer activity. (C) 2015 Elsevier Masson SAS. All rights reserved.
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