SYNTHESIS OF ARYLPIPERAZINES WITH A TERMINAL NAPHTHOTHIAZOLE GROUP AND THEIR EVALUATION ON 5-HT, DA AND ALPHA-RECEPTORS

Authors
PERRONE R BERARDI F COLABUFO NA TORTORELLA V FORNARETTO MG CACCIA C MCARTHUR RA
Citation
R. Perrone et al., SYNTHESIS OF ARYLPIPERAZINES WITH A TERMINAL NAPHTHOTHIAZOLE GROUP AND THEIR EVALUATION ON 5-HT, DA AND ALPHA-RECEPTORS, European journal of medicinal chemistry, 32(9), 1997, pp. 739-746
Citations number
34
Categorie Soggetti
Chemistry Medicinal
Journal title
European journal of medicinal chemistry → ACNP
ISSN journal
02235234
Volume
32
Issue
9
Year of publication
1997
Pages
739 - 746
Database
ISI
SICI code
0223-5234(1997)32:9<739:SOAWAT>2.0.ZU;2-J
Abstract
The synthesis, affinities for 5-HT1A, 5-HT2, D-1, D-2, alpha(1) and al pha(2) receptors and structure-activity relationships are described fo r a series of arylpiperazines substituted on the N-4 atom with an omeg a-(2-naphthothiazole)alkyl chain. The best affinity for 5-HT1A recepto rs was obtained for 1-(2-methoxyphenyl)piperazine derivatives with IC5 0 values in the range 3.2-12 nM; however, for all the reported compoun ds mixed 5-HT1A/D-2/alpha affinities were observed.