新型烯胺类化合物的合成与抗真菌活性研究.pdfVIP

新型烯胺类化合物的合成及抗真菌活性研究 a a1 a2 a a b 刘晓明 ，杨更亮 ，宋亚丽 ，刘杰杰 ，王洋 ，张冬暖 a河北省药物质量分析控制重点实验室, 河北大学药物化学与分子诊断省部共建教育部重点实验 室, 河北大学药学院, 保定 071002 b河北农业大学，保定 071001 摘要：以硫色满酮为起始原料合成一系列新型的烯胺类化合物。12个烯胺类化合物均未见报道， 1 13 其结构由 UV-vis，IR，HRMS， HNMR和 CNMR 确认。二维 NMR 证明这一类化合物在室温条件下是 以烯胺酮结构存在而不是西佛碱的结构。采用二倍浓度稀释法（平板法）测试各目标化合物的体 外抗真菌活性，实验选用两种临床上常用的致病真菌为测试菌株。 活性测试结果表明化合物 (反)-8-氯-3-((4-硝基苯基氨基)亚甲基)硫色满-4-酮 （4j）对新生隐球菌的最小抑菌浓度为32 -1 -1 µg·ml 优于对照药氟康唑 64 µg·ml 。 关键词：硫色满酮；烯胺；抗菌活性 Synthesis and Antifungal Activity of Some Novel Enaminones a a1 a2 a a b Liu Xiao-Ming , Yang Geng-Liang , Song Ya-Li , Liu Jie-Jie , WangYang , Zhang Dong-Nuan aKey Laboratory for Pharmaceutical Quality Control of Hebei Province, Key Laboratory of Medical Chemistry and Molecular Diagnosis, Ministry of Education, College of Pharmaceutical Sciences, Hebei University, Baoding, Hebei 071002, China b College of Science, Agricultural University of Hebei, Baoding, Hebei 071001, China Abstract ： A series of novel enaminones has been synthesized by using thiochroman-4-ones as the starting material. The structure of the new compounds is characterized by UV-vis, IR, HRMS, 1HNMR, and 13CNMR. 2D NMR spectroscopic studies revealed that these compounds exist in the keto-enamine form not Schiff base form at room temperature. The synthesized compounds were evaluated against two species of fungi in vitro by agar cup plate and micro-titration methods, respectively. The results of antifungal screening reveal that the MIC value of (E)-8-chloro-3-((4-nitrophenylamino)methylene)thiochroman-4-one (4j) against C.albicas is 32 µg·ml-1 while the contrast Fcz is 64 µg·ml-1.