Department of Biology and Chemistry, Universidad Tecnológica del Chocó, Quibdó, Colombia.
Arch Pharm (Weinheim). 2010 Jan;343(1):48-53. doi: 10.1002/ardp.200900187.
The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes using the microbroth dilution method. Compounds 4a and 4c showed antifungal activity, with compound 4a being the most active one. Compound 4a demonstrated to be fungicidal rather than fungistatic and selective activity against Cryptococcus neoformans and dermatophytes. MIC(100), MIC(80), and MIC(50) of 4a were determined against a panel of clinical isolates of C. neoformans showing ranges of MICs between 2 and 16 microg/mL.
本工作描述了新的 5-芳亚基-(Z)-2-二甲基氨基-1,3-噻唑-4-酮 4a-f 的合成和抗真菌评价，这些化合物是通过芳香醛 1 和脒基硫脲 2 的反应得到的，然后用 DMF 处理。所有化合物都采用微量肉汤稀释法对酵母、半知菌类和皮肤真菌进行了测试。化合物 4a 和 4c 表现出抗真菌活性，其中化合物 4a 的活性最强。化合物 4a 表现出杀菌而非抑菌作用，对新型隐球菌和皮肤真菌具有选择性活性。对一组新型隐球菌的临床分离株进行了 MIC(100)、MIC(80)和 MIC(50)的测定，MIC 值范围在 2 至 16 μg/mL 之间。
