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目的设计并合成2-芳基-2,3-二氢-4H-1,3-苯并噻嗪-4-酮类化合物,测定体外抗真菌活性、建立初步构效关系。方法以邻氨基苯甲酸为起始原料,经过重氮化及硫代反应制得二硫代水杨酸,再经过氯代、氨解、缩合等步骤制得目标化合物。采用2倍浓度稀释法,选用8种临床上常见的致病真菌为测试菌株,以氟康唑和伊曲康唑为阳性对照药,测试了目标化合物的体外抗真菌活性。结果与结论设计并合成了24个2-芳基-2,3-二氢-4H-1,3-苯并噻嗪-4-酮类化合物,目标化合物的结构经1H-NMR、MS确证;活性测试结果表明,目标化合物对测试真菌表现出不同程度的体外抑菌活性,所有化合物对红色毛藓菌和根霉菌的活性均好于阳性对照药。
OBJECTIVE To design and synthesize 2-aryl-2,3-dihydro-4H-1,3-benzothiazin-4-one compounds and determine the antifungal activity in vitro and to establish a preliminary structure-activity relationship. Methods Starting from anthranilic acid, dithio-salicylic acid was prepared through diazotization and thio-reaction, and then the target compound was obtained through the steps of chlorination, ammonolysis and condensation. The in vitro antifungal activity of the target compounds was tested by using 2 times concentration dilution method and 8 kinds of clinically common pathogenic fungi as test strains. Fluconazole and itraconazole were used as positive control drugs. RESULTS AND CONCLUSION Twenty-four 2-aryl-2,3-dihydro-4H-1,3-benzothiazinones were designed and synthesized. The structures of the target compounds were confirmed by 1H-NMR and MS. The results of the activity test showed that the target compounds showed different degree of antibacterial activity in vitro against the tested fungi, and all the compounds showed better activity against the Rhizopus sp. And Rhizopus sp. Than the positive control drugs.