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新型吡唑基-2,4-噻唑烷二酮类化合物的合成及抗炎和神经保护活性评价。

Synthesis and biological evaluation of novel pyrazolyl-2,4-thiazolidinediones as anti-inflammatory and neuroprotective agents.

机构信息

Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Alexandria, Alexandria, Egypt.

出版信息

Bioorg Med Chem. 2010 Mar 1;18(5):2019-28. doi: 10.1016/j.bmc.2010.01.021. Epub 2010 Jan 15.

Abstract

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.

摘要

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。

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