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目的:对硫色满酮并氮杂环衍生物进行体外抗真菌实验,筛选具有抗真菌活性的化合物并探讨其构效关系。方法:利用微量稀释法,以氟康唑和两性霉素B为阳性对照药,测定硫色满酮类并氮杂环衍生物对白色念珠菌、新生隐球菌、断发毛癣菌、红色毛癣菌、申克孢子丝菌(菌丝相)、石膏样小孢子菌、卡氏枝孢霉、黑曲霉、絮状毛癣菌的体外抑菌活性。结果:Bb, Da,Db,I,K对絮状表皮癣菌抑制作用显著,尤其Db的MIC低于两性霉素B;K对石膏样小孢子丝菌的MIC与两性霉素B相当。二甲氨基和甲氧基取代后,抗真菌比其他取代基化合物抗真菌活性高。结论:硫色满酮并氮杂环衍生物对常见致病真菌有一定的体外抑菌活性,值得深入研究。
OBJECTIVE: To investigate the antifungal activity of thiochromanone derivatives and their antifungal activities, and to explore their structure-activity relationship. Methods: Fluorescein and amphotericin B were used as positive control drugs to determine the inhibitory effect of sulfur-colored ketones and azole derivatives on Candida albicans, Cryptococcus neoformans, Trichophyton mentagrophytes, In vitro antibacterial activity of Spirulina, Mycophenolate sp. (Mycelial phase), Trichophyton mentagrophytes, Corynebacterium cardum, Aspergillus niger and Trichophyton floccosum in vitro. Results: The inhibitory effect of Bb, Da, Db, I and K on Epidermophyton floccosum was significant, especially that of Db was lower than that of amphotericin B; K had similar MIC to that of amphotericin B on G. gypseum. After the substitution of dimethylamino and methoxy, the antifungal activity is higher than that of other substituent compounds. CONCLUSION: Thiochromanone-aza-heterocyclic derivatives have certain antibacterial activity in vitro against common pathogenic fungi and deserve further study.