DERIVATIVES OF 2-ARYLCYCLOPROPYLAMINE - SYNTHESIS AND INTERACTIONS WITH 5-HT1A RECEPTORS

Authors
APPELBERG U MOHELL N HACKSELL U
Citation
U. Appelberg et al., DERIVATIVES OF 2-ARYLCYCLOPROPYLAMINE - SYNTHESIS AND INTERACTIONS WITH 5-HT1A RECEPTORS, Bioorganic & medicinal chemistry letters, 6(4), 1996, pp. 415-420
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
4
Year of publication
1996
Pages
415 - 420
Database
ISI
SICI code
0960-894X(1996)6:4<415:DO2-SA>2.0.ZU;2-Q
Abstract
A series of cis- and trans-derivatives of 2-aryl-N,N-dipropylcycloprop ylamines and 1-(2-arylcyclopropyl)-N,N-dipropylmethylamines were synth esized and evaluated for affinity at the 5-HT1A receptor. The key step in the syntheses was a cyclopropanation of cis- and trans-3-arylprope noic esters with diazomethane which proceeds with retention of the ste reochemistry. Methoxyphenyl)cyclopropyl]-N,N-dipropylmethylamine (32) had the highest 5-HT1A-receptor affinity (K-i = 58 nM) of the novel de rivatives.