Christina Papadopoulou, Athina Geronikaki, Dimitra Hadjipavlou-Litina
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引用次数: 83
摘要
合成了一系列噻唑- n -苯基哌嗪，并对其抗炎活性进行了测试。它们的RM值被确定为其亲脂性的表达。理论计算了它们的亲脂性，如clog P和logPsk。采用角叉菜胶致小鼠足跖水肿模型，研究了所合成化合物的抗炎作用。总的来说，所研究的化合物被发现是有效的抗炎剂(44-74.1%)。抗炎活性受合成化合物的一些结构特征的影响。利用定量构效关系方法(QSAR)对其生物活性与理化参数进行了关联分析。
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 RM 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).
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