Russian Journal of Bioorganic Chemistry ( IF 1.1 ) Pub Date : 2021-08-21 , DOI: 10.1134/s1068162021040051 T. I. Chaban 1 , V. V. Ogurtsov 1 , V. T. Foliush 2 , V. S. Matiychuk 2
Abstract—
By the reaction of chloroacetamidothiazole with 5-aryltetrazoles and 5-mercaptotetrazoles 2-(5-aryltetrazol-2-yl)- and 2-(1H-tetrazol-5-ylsulfanyl)-N-thiazol-2-ylacetamides were prepared. The study of the anti-inflammatory properties of the synthesized compounds was carried out. Compounds have been identified, whose activity exceeds the reference drug ibuprofen. Molecular docking to cyclooxygenase-1 and cyclooxygenase-2 was carried out and it was shown that 2-[1-(2,5-dimethylphenyl)-1H-tetrazol-5-ylsulfanyl]-N-thiazol-2-ylacetamide has the highest affinity for the active center of the cyclooxygenase.
中文翻译:
2-(5-Aryltetrazol-2-yl)-和2-(1H-Tetraazol-5-ylsulphanyl)-N-Thiazol-2-ylacetamides 的合成、抗炎特性和分子对接
摘要——
通过氯代乙酰氨基噻唑与5-芳基四唑和5-巯基四唑的反应,制备了2-(5-芳基四唑-2-基)-和2-( 1H-四唑-5-基硫烷基) -N-噻唑-2-基乙酰胺。对合成化合物的抗炎特性进行了研究。已鉴定出活性超过参考药物布洛芬的化合物。与环氧合酶-1和环氧合酶-2进行分子对接,结果表明2-[1-(2,5-二甲基苯基) -1H-四唑-5-基硫烷基] -N-噻唑-2-基乙酰胺具有对环氧合酶活性中心的亲和力最高。