A convenient synthesis by microwave heating and pharmacological evaluation of novel benzoyltriazole and saccharine derivatives as 5-HT1A receptor ligands

被引：37

作者：

Caliendo, G

Fiorino, F

Perissutti, E

Severino, B

Scolaro, D

Gessi, S

Cattabriga, E

Borea, PA

Santagada, V

机构：

[1] Univ Naples Federico II, Dipartimento Chim Farmaceut & Tossicol, I-80131 Naples, Italy

[2] Univ Ferrara, Dipartimento Med Clin & Sperimentale, Sez Farmacol, I-44100 Ferrara, Italy

来源：

EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES | 2002年 / 16卷 / 1-2期

关键词：

5-HT receptors; microwave; medicinal chemistry; benzoyltriazole; saccharine;

D O I：

10.1016/S0928-0987(02)00045-3

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A series of novel 1,2,3-4-benzoyltriazole and saccharine derivatives were designed and synthesized by microwave heating. They were evaluated on a battery of receptors, including serotonin 5-HT1A, 5-HT2A, and 5-HT2C, and the most interesting compounds were further evaluated on dopaminergic D-1, D-2 and adrenergic alpha(1), alpha(2) receptors. Conventional and microwave heating of the reactions were compared. Synthesis by microwave heating gave the desired compounds in better yields than those obtained by conventional heating. The overall times for the syntheses were considerably reduced. All compounds displayed moderate affinity for 5-HT1A receptor. The most interesting compound 33 showed a high affinity (K-i=93 nM) which was combined with no affinity on the other receptors considered. (C) 2002 Elsevier Science BY All rights reserved.

引用

页码：15 / 28

页数：14

共 26 条

[11] 4-(4-fluorobenzoyl)-1-[2-(4-iodo-2,5-dimethoxyphenyl)ethyl]piperidine and its derivatives:: synthesis and affinity at 5-HT2A, 5-HT2B and 5-HT2C serotonin receptors [J].