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Synthesis and biological evaluation of new thiazolyl/benzothiazolyl-amides, derivatives of 4-phenyl-piperazine.
- 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).
- Subjects :
- Amides chemical synthesis
Animals
Anti-Inflammatory Agents chemical synthesis
Benzothiazoles chemical synthesis
Carrageenan
Disease Models, Animal
Edema chemically induced
Female
Male
Mice
Mice, Inbred AKR
Molecular Structure
Quantitative Structure-Activity Relationship
Regression Analysis
Thiazoles chemical synthesis
Amides pharmacology
Anti-Inflammatory Agents pharmacology
Benzothiazoles pharmacology
Edema prevention & control
Piperazines chemistry
Thiazoles pharmacology
Subjects
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