1,2,3-triazolo[1,5-a][1,4]- and 1,2,3-triazolo[1,5-a][1,5]benzodiazepine derivatives: synthesis and benzodiazepine receptor binding
1,2,3-triazolo[1,5-a][1,4]- and 1,2,3-triazolo[1,5-a][1,5]benzodiazepine derivatives: synthesis and benzodiazepine receptor binding
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DOI：
10.1016/s0014-827x(98)00025-1
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发表时间：
1998-04-01
期刊：
影响因子：
--
通讯作者：
Barili, PL
中科院分区：
文献类型：
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作者：
Bertelli, L;Biagi, G;Barili, PL
本文报道了新的1,2,3-三唑[1,4]苯二氮卓和1,2,3-三唑[1,5]苯二氮卓衍生物的合成及其对苯二氮卓受体的评价，通过将中心环的氮原子从3、4位移动到5位，得到最有效的化合物6a （K-i = 150 nM）。二氮平环（7a）的n -甲基化降低受体结合。苯环上氯原子的引入使K-i值（6b）加倍，而n -甲基化（7b）仍未改变K-i值。(C) 1998 Elsevier Science S.A.版权所有
This paper reports the synthesis of new 1,2,3-triazolo[1,4]benzodiazepine and 1,2,3-triazolo[1,5]benzodiazepine derivatives and their evaluation toward benzodiazepine receptors, Receptor affinity gradually and remarkably increases by moving the nitrogen atom of the central ring from position 3 through 4 to position 5, to give the most effective compound 6a (K-i = 150 nM). N-methylation of the diazepine ring (7a) lowers receptorial binding. Introduction of a chlorine atom on the benzene ring doubles the K-i value (6b) which remains unaltered by the N-methylation (7b). (C) 1998 Elsevier Science S.A. All rights reserved.