Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.
Bioorg Med Chem. 2010 Mar 1;18(5):2019-28. doi: 10.1016/j.bmc.2010.01.021. Epub 2010 Jan 15.
Novel pyrazolyl-2,4-thiazolidinediones were prepared via the reaction of appropriate pyrazolecarboxaldehydes with 2,4-thiazolidinediones and substituted benzyl-2,4-thiazolidinediones. The resultant compounds were first evaluated for their anti-inflammatory and neuroprotective properties in vitro. The active compounds were further studied in vivo by using the formalin-induced paw edema and the turpentine oil-induced granuloma pouch bioassays. We identified four novel compounds that showed protective effects in vitro at non-toxic concentrations, and were also effective in the animal models of acute and sub-acute inflammation.
新型吡唑基-2,4-噻唑烷二酮类化合物是通过适当的吡唑甲醛与 2,4-噻唑烷二酮和取代的苄基-2,4-噻唑烷二酮反应制备的。所得化合物首先在体外评估其抗炎和神经保护特性。通过使用福马林诱导的爪肿胀和松节油诱导的肉芽肿囊生物测定，对活性化合物进行了进一步的体内研究。我们鉴定了四种新型化合物，它们在非毒性浓度下显示出体外保护作用，并且在急性和亚急性炎症的动物模型中也有效。
