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合成及药理评价新型系列 3-芳基-2-(2-取代-4-甲基噻唑-5-基)噻唑烷-4-酮作为潜在的抗炎和抗菌药物。

Synthesis and pharmacological evaluation of a novel series of 3-aryl-2-(2-substituted-4-methylthiazole-5-yl)thiazolidin-4-one as possible anti-inflammatory and antimicrobial agents.

机构信息

Department of Chemistry, HPT Arts and RYK Science College, Vidyanagari, Nashik 422005, India.

出版信息

Bioorg Med Chem Lett. 2012 Oct 15;22(20):6373-6. doi: 10.1016/j.bmcl.2012.08.073. Epub 2012 Aug 25.

Abstract

A new series of 3-aryl-2-(2-aryl/benzyl-4-methylthiazole-5-yl)thiazolidin-4-one was synthesized by condensation of 2-aryl/benzyl-4-methylthiazole-5-carbaldehyde, aromatic amines and thioglycolic acid in toluene. All the synthesized compounds are characterized by IR, NMR and elemental or mass analysis. Sixteen out of the newly synthesized compounds were screened for in vivo anti-inflammatory activity using carrageenan-induced rat paw edema method. Some of the synthesized compounds exhibited good anti-inflammatory activity compared with indomethacin. The synthesized compounds were also evaluated for their in vitro antimicrobial activity. Some of the compounds showed mild antibacterial activity while most of the compounds showed good antifungal activity.

摘要

通过 2-芳基/苄基-4-甲基噻唑-5-甲醛、芳香胺和巯基乙酸在甲苯中的缩合反应,合成了一系列新的 3-芳基-2-(2-芳基/苄基-4-甲基噻唑-5-基)噻唑烷-4-酮。所有合成的化合物均通过 IR、NMR 和元素或质量分析进行了表征。十六种新合成的化合物通过角叉菜胶诱导的大鼠足肿胀法进行了体内抗炎活性筛选。与吲哚美辛相比,一些合成的化合物表现出良好的抗炎活性。还评估了合成化合物的体外抗菌活性。一些化合物表现出轻微的抗菌活性,而大多数化合物表现出良好的抗真菌活性。

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