Series of new derivatives of ninhydrin, isatin, and 4-hydroxy-1,3-thiazine-2,6-dione were synthesized. Their antimicrobial activity against opportunistic microflora of Staphylococcus aureus and Pseudomonas aeruginosa isolated from neurotrophic ulcers of leprosy patients was studied. Antibacterial activity against S. aureus was observed for derivatives of chalcone (MIC 2.31 ± 0.99 and 8.0 ± 2.83 μg/mL), benzofuran (MIC 3.5 ± 1.66 μg/mL), imines (MIC 0.56 ± 0.16 and 3.01 ± 1.68 μg/mL), and indene (MIC 1.38 ± 0.38 μg/mL). Derivatives of imine (MIC 0.25 ± 0.05 and 0.63 ± 0.26 μg/mL) and indene also exhibited pronounced inhibitory effects against P. aeruginosa. Bactericidal effects on both cultures were observed for 5-(1E)-1-[2-(1-benzothiophen-2-yl)hydrazinylidene]-ethyl}-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione. An indene derivative with a morpholine fragment showed a pronounced bactericidal effect (MBC 2.3 ± 0.58 μg/mL) on the growth of P. aeruginosa culture.
研究人员合成了一系列
茚三酮、
靛红和
4-羟基-
1,3-噻嗪-2,6-二酮的新衍
生物。研究了它们对从麻风病人神经营养性溃疡中分离出来的
金黄色葡萄球菌和绿脓杆菌等机会性微
生物的抗菌活性。发现
查尔酮衍
生物(MIC 2.31 ± 0.99 和 8.0 ± 2.83 μg/mL)、
苯并呋喃衍
生物(MIC 3.5 ± 1.66 μg/mL)、
亚胺衍
生物(MIC 0.56 ± 0.16 和 3.01 ± 1.68 μg/mL)和
茚衍
生物(MIC 1.38 ± 0.38 μg/mL)对
金黄色葡萄球菌具有抗菌活性。
亚胺的衍
生物(MIC 0.25 ± 0.05 和 0.63 ± 0.26 μg/mL)和
茚对
铜绿假单胞菌也有明显的抑制作用。5-(1E)-1-[2-(1-benzothiophen-2-yl)hydrazinylidene]-ethyl}-4-hydroxy-2H-1,3-thiazine-2,6(3H)-dione 对两种培养物都有杀菌作用。带有吗啉片段的
茚衍
生物对
铜绿假单胞菌的生长有明显的杀菌作用(MBC 2.3 ± 0.58 μg/mL)。