Derivatives of 2-arylcyclopropylamine: Synthesis and interactions with 5-HT1A receptors.

被引：5

作者：

Appelberg, U

Mohell, N

Hacksell, U

机构：

[1] UNIV UPPSALA,CTR BIOMED,DEPT ORGAN PHARMACEUT CHEM,S-75123 UPPSALA,SWEDEN

[2] ASTRA ARCUS AB,PRECLIN RES & DEV,DEPT MOLEC PHARMACOL,S-15185 SODERTALJE,SWEDEN

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 04期

关键词：

D O I：

10.1016/0960-894X(96)00045-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of cis- and trans-derivatives of 2-aryl-N,N-dipropylcyclopropylamines and 1-(2-arylcyclopropyl)-N,N-dipropylmethylamines were synthesized and evaluated for affinity at the 5-HT1A receptor. The key step in the syntheses was a cyclopropanation of cis- and trans-3-arylpropenoic esters with diazomethane which proceeds with retention of the stereochemistry. cis-1-[2-(3-Methoxyphenyl)cyclopropyl]-N,N-dipropylmethylamine (32) had the highest 5-HT1A-receptor affinity (K-i = 58 nM) of the novel derivatives.

引用

页码：415 / 420

页数：6

共 11 条

[1] STRUCTURAL FACTORS OF IMPORTANCE FOR 5-HYDROXYTRYPTAMINERGIC ACTIVITY - CONFORMATIONAL PREFERENCES AND ELECTROSTATIC POTENTIALS OF 8-HYDROXY-2-(DI-N-PROPYLAMINO)TETRALIN (8-OH-DPAT) AND SOME RELATED AGENTS [J].