Synthesis and antimicrobial evaluation of new 3-alkyl/aryl-2-[((α,α-diphenyl-α-hydroxy)acetyl)hydrazono]-5-methyl-4-thiazolidinones
作者:Nuray Ulusoy Güzeldemirci、Eser Ilhan、Ömer Küçükbasmaci、Dilek Satana
DOI:10.1007/s12272-010-2221-y
日期:2010.1
New 4-thiazolidinone derivatives of benzilic acid (α,α-diphenyl-α-hydroxyacetic acid) have been synthesized and evaluated for antibacterial and antifungal activities. The reaction of 1- (α,α-diphenyl-α-hydroxy)acetyl-4-alkyl/arylthiosemicarbazides with ethyl 2-bromopropionate gave 3-alkyl/aryl-2-[((α,α-diphenyl-α-hydroxy)acetyl)hydrazono]-5-methyl-4-thiazolidinone derivatives. Their antibacterial and antifungal activities were evaluated against S. aureus ATCC 29213, P. aeruginosa ATCC 27853, E. coli ATCC 25922, C. albicans ATCC 10231, C. parapsilosis ATCC 22019, C. krusei ATCC 6258, T. mentagrophytes var. erinacei NCPF 375, M. gypseum NCPF 580 and T. tonsurans NCPF 245. 3e, 3f, 3g and 3h showed the highest antibacterial activity. Particularly 3a and 3e showed the highest antifungal activities against C. parapsilosis ATCC 22019, T. tonsurans NCPF 245 and M. gypseum NCPF 580.
新型4-噻唑啉酮衍生物的苯乙酸(α,α-二苯基-α-羟基乙酸)已被合成并评估了其抗菌和抗真菌活性。1-(α,α-二苯基-α-羟基)乙酰-4-烷基/芳香族噻唑氨基脲与乙基2-溴丙酸酯反应,生成3-烷基/芳香族-2-[((α,α-二苯基-α-羟基)乙酰)肼佐] -5-甲基-4-噻唑啉酮衍生物。它们的抗菌和抗真菌活性在以下菌株中进行了评估:金黄色葡萄球菌 ATCC 29213、铜绿假单胞菌 ATCC 27853、大肠杆菌 ATCC 25922、白色念珠菌 ATCC 10231、副念珠菌 ATCC 22019、克鲁斯念珠菌 ATCC 6258、松毛念珠菌 NCPF 375、石膏毛霉 NCPF 580 和小孢子菌 NCPF 245。3e、3f、3g和3h表现出最高的抗菌活性。特别是3a和3e在对副念珠菌 ATCC 22019、小孢子菌 NCPF 245 和石膏毛霉 NCPF 580 的抗真菌活性中表现最佳。