SAR studies of capsazepinoid bronchodilators 3:: The thiourea part (coupling region) and the 2-(4-chlorophenyl)ethyl moiety (C-region)
SAR studies of capsazepinoid bronchodilators 3:: The thiourea part (coupling region) and the 2-(4-chlorophenyl)ethyl moiety (C-region)
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DOI：
10.1016/j.bmc.2007.11.056
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发表时间：
2008-03-01
影响因子：
3.5
通讯作者：
Sterner, Olov
中科院分区：
文献类型：
--
作者：
Berglund, Magnus;Dalence-Guzman, Maria F.;Sterner, Olov
辣椒平的某些衍生物和类似物是人小气道中支气管收缩的有效体外抑制剂。在研究效力对硫脲部分（偶联区）和2-（4-氯苯基）乙基部分（G区）中辣椒类物质的结构特征的依赖性期间，发现在B环和G区之间具有硫脲或酰胺连接的辣椒类物质通常具有良好的支气管舒张活性，而脲是不太有吸引力的选择。此外，还表明具有2-（苯基）乙基衍生物作为C区的1，2，3，4-四氢异喹啉比具有辛基的那些有效得多，而发现2，3，4，5-四氢-1H-2-苯并氮杂卓对G区的性质更不敏感。(C)2007爱思唯尔有限公司保留所有权利。
Certain derivatives and analogues of capsazepine are potent in vitro inhibitors of bronchoconstriction in human small airways. During an investigation of the dependency of the potency on the structural features of the capsazepinoids in the thiourea moiety (coupling region) and the 2-(4-chlorophenyl)ethyl moiety (Gregion), it was revealed that capsazepinoids with a thiourea or an amide link between the B-ring and the Gregion in general have a good bronchorelaxing activity, while urea is a less attractive choice. Further, it was shown that 1,2,3,4-tetrahydroisoquinolines with a 2-(phenyl)ethyl derivative as the C-region are considerably more potent than those with an octyl group, while 2,3,4,5-tetrahydro-1H-2-benzazepines were found to be more insensitive to the nature of the Gregion. (C) 2007 Elsevier Ltd. All rights reserved.