Synthesis and biological evaluation of new thiazolyl/benzothiazolyl-amides, derivatives of 4-phenyl-piperazine.
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).
Papadopoulou
Christina
C
Department of Pharmaceutical Chemistry, School of Pharmacy University Campus, Aristotle University, Thessaloniki 54124, Greece.
Geronikaki
Athina
A
Hadjipavlou-Litina
Dimitra
D
D000577:Amides / Q000138:chemical synthesis / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D052160:Benzothiazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D002351:Carrageenan; D004195:Disease Models, Animal; D004487:Edema / Q000139:chemically induced / Q000517:prevention & control*; D005260:Female; D008297:Male; D051379:Mice; D008806:Mice, Inbred AKR; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry*; D021281:Quantitative Structure-Activity Relationship; D012044:Regression Analysis; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology*
D000577:Amides; D000893:Anti-Inflammatory Agents; D052160:Benzothiazoles; D010879:Piperazines; D013844:Thiazoles; D002351:Carrageenan