Synthesis of new 5-phenyl[1,2,4]triazole derivatives as ligands for the 5-HT1A serotonin receptor

被引：21
|
作者：
Salerno, L
Siracusa, M
Guerrera, F
Romeo, G
Pittala, V
Modica, M
Mennini, T
Russo, F [1 ]
机构：
[1] Univ Catania, Dipartimento Sci Farmaceut, Fac Farm, Viale Andrea Doria 6, I-95125 Catania, Italy
[2] Ist Ric Farmacol Mario Negri, I-20157 Milan, Italy
来源：
ARKIVOC | 2004年
关键词：
5-phenyl[1,2,4]triazole; 5-HT1A serotonin receptor; alpha(1)-adrenoceptor subtypes; triazole ring alkylation;
D O I：
10.3998/ark.5550190.0005.527
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
A series of 4-amino-3-[[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl] thio]-5-(substituted phenyl)[1,2,4] triazoles(5a-f) and the isomeric 4-amino-2-[2-[4-(2-methoxyphenyl)-1-piperazinyl] ethyl]-5-(substitutedphenyl)-2,4-dihydro-3H[1,2,4] triazole-3-thiones (6a-f) and a series of 3-[[2-[4-(2-methoxy or 2- nitrophenyl) 1-piperazinyl] ethyl] thio]-5-(substituted phenyl)[1,2,4] triazoles (8a-i) were synthesized with the aim of obtaining new selective 5-HT1A ligands, with reduced affinity for the alpha(1)-adrenoceptor subtypes. New compounds were tested in radioligand binding experiments where many of them showed a preferential affinity for the 5-HT1A receptor.
引用
收藏
页码：312 / 324
页数：13
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