NOVEL BENZOTHIAZOLIN-2-ONE AND BENZOXAZIN-3-ONE ARYLPIPERAZINE DERIVATIVES WITH MIXED 5HT(1A) D-2 AFFINITY AS POTENTIAL ATYPICAL ANTIPSYCHOTICS/

Authors
TAVERNE T DIOUF O DEPREUX P POUPAERT JH LESIEUR D GUARDIOLALEMAITRE B RENARD P RETTORI MC CAIGNARD DH PFEIFFER B
Citation
T. Taverne et al., NOVEL BENZOTHIAZOLIN-2-ONE AND BENZOXAZIN-3-ONE ARYLPIPERAZINE DERIVATIVES WITH MIXED 5HT(1A) D-2 AFFINITY AS POTENTIAL ATYPICAL ANTIPSYCHOTICS/, Journal of medicinal chemistry, 41(12), 1998, pp. 2010-2018
Citations number
48
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
41
Issue
12
Year of publication
1998
Pages
2010 - 2018
Database
ISI
SICI code
0022-2623(1998)41:12<2010:NBABAD>2.0.ZU;2-I
Abstract
Since it was known that 5HT properties (5HT(1A) agonism or 5HT(2A) ant agonism) combined with D-2 antagonism may lead to atypical antipsychot ic drugs, a series of 19 benzothiazolin-2-one and benzoxazin-3-one der ivatives possessing the arylpiperazine moiety Was prepared, and their binding profiles were investigated. All tested compounds displayed ver y high affinities for the 5HT(1A) and Da receptors. Therefore, further pharmacological studies were carried out on selected compounds (24, 2 7, 30, 46, and 47). This evaluation in rats clearly revealed potent an tipsychotic properties along with a decrease of extrapyramidal side ef fects. These derivatives are currently under preclinical development.