1. 河北大学 a. 药学院 河北省药品质量控制重点实验室; b. 教育部药物化学与分子诊断重点实验室，河北 保定 071002
Synthesis and Antifungal Activities of Novel Thiochromanone Derivatives Containing 1,3,4-Thiadiazole
LIANG Guo-chao1a,1b, ZHOU Guan1a,1b, ZHONG Yi-fan1a,1b, HAN Xiao-yan1a,1b, SONG Ya-li1a,1b
a. Key Laboratory for Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical; b. Key Laboratory of Medicinal Chemistry and Molecular Diagnosis, Ministry of Education, 1. Hebei University, Baoding 071002, China
Abstract：4-Thiochromane-2-carboxylic acid derivatives(2a~2d) were prepared by Michael addition reaction of substituted thiophenol with maleic anhydride. 2-(5-amino-1,3,4-thiadiazol-2-yl)thiochroman-4-one derivatives(3a~3d) were prepared by acylation reaction of 2a~２2d with thiosemicarbazide, respectively. Fourteen novel thiochromanone derivatives(5a~5n) containing 1,3,4-thiadiazole were synthesized by reaction of 3a~3d with acyl chloride. The structures were characterized by 1H NMR, 13C NMR and HR-ESI-MS. The antifungal activities of 5a~5n were investigated by micro dilution method. The results showed that some derivatives exhibited better antifungal activities on Epidermophyton floccosum and Mucor racemosus than Fluconazole.
2015, Vol. 23 
