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Synthesis and biological evaluation of new thiazolyl/benzothiazolyl-amides, derivatives of 4-phenyl-piperazine.

Authors :
Papadopoulou C
Geronikaki A
Hadjipavlou-Litina D
Source :
Farmaco (Societa chimica italiana : 1989) [Farmaco] 2005 Nov-Dec; Vol. 60 (11-12), pp. 969-73. Date of Electronic Publication: 2005 Jul 22.
Publication Year :
2005

Abstract

A series of thiazolyl-N-phenyl piperazines has been synthesised and tested for anti-inflammatory activity. Their R(M) values were determined as an expression of their lipophilicity. Theoretical calculation of their lipophilicity, as clog P and logPsk also performed. The effect of the synthesised compounds on inflammation, using the carrageenin induced mouse paw oedema model was studied. In general, the studied compounds were found to be potent anti-inflammatory agents (44-74.1%). Anti-inflammatory activity was influenced by some structural characteristics of the synthesised compounds. An attempt was made to correlate their biological activity with some physicochemical parameters using a quantitative structure-activity relationship approach (QSAR).

Details

Language :
English
ISSN :
0014-827X
Volume :
60
Issue :
11-12
Database :
MEDLINE
Journal :
Farmaco (Societa chimica italiana : 1989)
Publication Type :
Academic Journal
Accession number :
16040029
Full Text :
https://doi.org/10.1016/j.farmac.2005.06.014