Dalence-Guzmán María F, Berglund Magnus, Skogvall Staffan, Sterner Olov
Division of Organic Chemistry, Lund University, PO Box 124, SE-221 00 Lund, Sweden; Centro de Tecnologia Agroindustrial, Facultad de Ciencias y Tecnologia, Universidad Mayor de San Simón, Cochabamba, Bolivia.
Bioorg Med Chem. 2008 Mar 1;16(5):2499-512. doi: 10.1016/j.bmc.2007.11.055. Epub 2007 Nov 28.
Capsazepine as well as its derivatives and analogues are general inhibitors of constriction of human small airways. From a systematic variation of the capsazepine structure, divided into four regions, SARs were established. This part concerns the catechol moiety of the A-ring as well as the 2,3,4,5-tetrahydro-1H-2-azepine moiety (the B-ring) of capsazepine. It is revealed that a conformational constrain (as a fused ring) is important and that compounds with a six-membered B-ring (as a 1,2,3,4-tetrahydroisoquinoline) in general are more potent than the corresponding isoindoline, 2,3,4,5-tetrahydro-1H-2-benzazepine and 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives.
辣椒平及其衍生物和类似物是人类小气道收缩的一般抑制剂。通过对辣椒平结构进行系统的变化（分为四个区域），建立了构效关系。这部分涉及辣椒平A环的儿茶酚部分以及2,3,4,5-四氢-1H-2-氮杂卓部分（B环）。结果表明，构象限制（作为稠环）很重要，并且一般来说，具有六元B环（作为1,2,3,4-四氢异喹啉）的化合物比相应的异吲哚啉、2,3,4,5-四氢-1H-2-苯并氮杂卓和2,3,4,5-四氢-1H-3-苯并氮杂卓衍生物更有效。
