Department of Organic Chemistry, Chemical Diversity Research Institute, Khimki, Moscow Reg, Russia.
Arch Pharm (Weinheim). 2009 Dec;342(12):740-7. doi: 10.1002/ardp.200900056.
Synthesis, biological evaluation, and structure-activity relationships (SAR) for a series of novel gamma-carboline analogues of Dimebon are described. Among the studied compounds, tetrahydro-gamma-carboline 5b (2,8-dimethyl-5-[cis-2-pyridin-3-ylvinyl]-2,3,4,5-tetrahydro-carboline) has been identified as the most potent small molecule antagonist, in particular against histamine H(1) and serotonin 5-HT(6) receptors (IC(50) < 0.45 microM and IC(50) = 0.73 microM, respectively). A thorough comparative SAR study performed for the tested compounds has revealed significant correlations between the nature of side substituents and the related antagonistic activity.
描述了一系列新型二美苯类似物的伽马-咔啉的合成、生物评价和构效关系（SAR）。在所研究的化合物中，四氢-伽马-咔啉 5b（2,8-二甲基-5-[顺式-2-吡啶-3-基乙烯基]-2,3,4,5-四氢-咔啉）已被确定为最有效的小分子拮抗剂，特别是针对组胺 H（1）和 5-羟色胺 5-HT（6）受体（IC（50）<0.45 microM 和 IC（50）= 0.73 microM，分别）。对测试化合物进行的全面比较 SAR 研究表明，侧取代基的性质与相关拮抗活性之间存在显著相关性。
