新型酮洛芬硫脲衍生物的设计、合成、硅学研究和抗炎评价

Rafid M. Hashim, Y. Y. Z. Farid
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引用次数: 0

摘要

本研究设计并合成了六种新的酮洛芬硫脲衍生物,以提高 COX-2 酶的选择性。通过光谱分析确认了这些衍生物的化学结构。研究了这些衍生物的体内和体外抗炎活性。结果表明,化合物 B4 的活性最高。 根据计算方法的预测,新衍生物还具有药物亲和性和胃吸收性。 上述结果表明,合成的化合物作为潜在的选择性 COX-2 抑制剂值得进一步研究。
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Design, Synthesis, In Silico Study and Anti-Inflammatory Evaluation of New Ketoprofen Thiourea Derivatives
The In the current study, six new derivatives of ketoprofen thiourea were designed and synthesized In order to enhance COX-2 enzyme selectivity. The chemical structures of these derivatives were confirmed by spectral analysis. The anti-inflammatory activities of these derivatives was investigated insilico and in vivo. The results revealed that compound B4 were the most active.  The new derivatives also showed drug-likeness and gastric absorption as predicted by computational methods.  These results above indicated that the synthesized compounds deserve additional investigation as potential selective COX-2 inhibitors.
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