Thiochromone compound, synthetic method and application thereof in preparing antifungal medicaments

Abstract

The invention relates to a thiochromone compound, which has the structure as right: wherein R1 is five-membered nitrogen-containing aromatic heterocycle substituted by hydrogen, methyl, nitryl or cyanThe invention relates to a thiochromone compound, which has the structure as right: wherein R1 is five-membered nitrogen-containing aromatic heterocycle substituted by hydrogen, methyl, nitryl or cyanep fungal infection, low toxicity, good stability and broad antifungal spectrum.ep fungal infection, low toxicity, good stability and broad antifungal spectrum.o; R2 is aliphatic alkyl of C1 to C12 or unsubstituted five-membered or six-membered aromatic ring aliphatic alkyl or five-membered or six-membered aromatic ring aliphatic alkyl selectively substituteo; R2 is aliphatic alkyl of C1 to C12 or unsubstituted five-membered or six-membered aromatic ring aliphatic alkyl or five-membered or six-membered aromatic ring aliphatic alkyl selectively substituted by amino group, methyl, trifluoromethyl, trifluoromethoxy, nitryl, halogen and cyano; R3 is alkyl, hydrogen, fluorine, chlorine, bromine or iodine of C1 to C4; R4 is hydrogen, fluorine, chlorine, brd by amino group, methyl, trifluoromethyl, trifluoromethoxy, nitryl, halogen and cyano; R3 is alkyl, hydrogen, fluorine, chlorine, bromine or iodine of C1 to C4; R4 is hydrogen, fluorine, chlorine, bromine, iodine or five-membered or six-membered heterocycle containing nitrogen; and R5 and R6 are hydrogen, fluorine, chlorine, bromine, iodine, alkyl of C1 to C4, hydroxyl, oxyl of C1 to C4, cyano, nomine, iodine or five-membered or six-membered heterocycle containing nitrogen; and R5 and R6 are hydrogen, fluorine, chlorine, bromine, iodine, alkyl of C1 to C4, hydroxyl, oxyl of C1 to C4, cyano, nitryl, amino group or amino group substituted by alkyl of C1 to C4. The compound has application in preparing antifungal medicaments, strong bacteriostatic activity for common pathogenic fungus and deitryl, amino group or amino group substituted by alkyl of C1 to C4. The compound has application in preparing antifungal medicaments, strong bacteriostatic activity for common pathogenic fungus and de

Description

Background technique In the past two decades, with the application of a large number of broad-spectrum antibiotics, the development of bone marrow organ transplantation, the application of glucocorticoids and immunosuppressants, catheter interventional therapy, especially the prevalence of AIDS, candidemia and systemic aspergillosis, etc. Systemic fungal infections gradually increased. In particular, the incidence of invasive fungal infections is increasing, causing serious harm to human health. The most common pathogens causing invasive fungal infections include Candida species (70%-90% of invasive fungal infection cases) and Aspergillus (10%-20%). Among immunocompromised AIDS patients, the incidence of life-threatening systemic fungal infections is increasing rapidly. According to their structure and mechanism of action, antifungal drugs can be divided into five categories: polyene antifungal drugs, echinocandin antifungal drugs, pyrimidine antifungal drugs, allylamine ant...

AI Technical Summary

Problems solved by technology

The above chemical modification methods mainly focus on the 1, 3, and 4 positions of thiochromone. The modified compounds can only increase the antibacterial activity against specific fungi, and cannot meet the requirements of broad-spectrum antifungal activity.

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