High potent and selective arylpiperazine derivatives as ligands for the 5-HT1A receptor

被引：14
|
作者：
Modica, M
Santagati, M
Santagati, A
Russo, F
Cagnotto, A
Goegan, M
Mennini, T
机构：
[1] Catania Univ, Dipartimento Sci Farmaceut, I-95125 Catania, Italy
[2] Mario Negri Inst Pharmacol Res, I-20157 Milan, Italy
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 10期
关键词：
D O I：
10.1016/S0960-894X(00)00165-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
This paper reports the synthesis and affinities on the 5HT(1A) versus the alpha(1)A receptors of new arylpiperazinylalkylthiothienopyrimidine and thiadiazole derivatives 16-24. Arylpiperazines 16-23 show affinities values in the nanomolar range for the 5HT(1A) receptor. The compound 16 is highly potent (K-i 0.26 nM, selectivity 28), the derivatives 20 and 21 are less potent, but highly selective (K-i 9.40 and 5.06 nM, selectivity 207 and 73, respectively). (C) 2000 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：1089 / 1092
页数：4
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