2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers
2-Aminothiophene-3-carboxylates and carboxamides as adenosine A1 receptor allosteric enhancers
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DOI：
10.1016/j.bmc.2005.11.018
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发表时间：
2006-04-01
影响因子：
3.5
通讯作者：
Scammells, PJ
中科院分区：
文献类型：
--
作者：
Nikolakopoulos, G;Figler, H;Scammells, PJ
用Gewald合成法合成了3个系列的2-氨基-4，5，6，7-四氢苯并[B]噻吩和2-氨基-5，6，7，8-四氢环庚[B]噻吩的3-羧酸酯和3-酰胺酯，并评价了它们作为AIAR变构增强剂的活性。这些类别的化合物的结构-活性关系进行了描述。许多化合物，特别是7 b，比PD 81，723（1）更有效。(c)2005爱思唯尔有限公司保留所有权利。
Three series of 2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene and 2-amino-5,6,7,8-tetrahydrocyclohepta[b]thiophenes with 3-carboxylates and carboxamides have been prepared using the Gewald synthesis and evaluated as AIAR allosteric enhancers. The structure-activity relationships of these classes of compound are described. A number of compounds, notably 7b, are more potent and efficacious than PD81,723 (1). (c) 2005 Elsevier Ltd. All rights reserved.