Department of Chemistry, Faculty of Sciences, Persian Gulf University, Bushehr, 75169, Iran.
Department of Chemistry, Faculty of Sciences, Persian Gulf University, Bushehr, 75169, Iran.
Microb Pathog. 2019 May;130:95-99. doi: 10.1016/j.micpath.2019.03.002. Epub 2019 Mar 6.
Xanthene derivatives are well known for their effective biological activities. In search of effective antibacterial agents, the spiro[indoline3,9-xanthene]-trione (A) and hydroxy-spiro[indoline-3,9-xanthene]-trione (B), were synthesized and tested for in vitro antibacterial activity against Staphylococcus aureus and Escherichia coli. Furthermore, the synthesized compounds were tested in vitro and in silico for their anticholinesterase activities. The anticholinesterase activities for six substitutes of the hydroxy derivative (B1-B6) were also studied through the molecular docking. All concentrations of compounds presented a dose-dependent antibacterial activity. The docking results showed that all compounds are more constant than the galantamine. Amongst, compound B1 exhibited the minimum binding energy in both AChE and BChE enzymes. Results indicate the importance of xanthene derivatives as potential antibacterial and anticholinesterases agents.
香豆素衍生物以其有效的生物活性而闻名。在寻找有效的抗菌剂的过程中，合成了螺[吲哚啉-3,9-香豆素]-1,3-二酮（A）和羟基螺[吲哚啉-3,9-香豆素]-1,3-二酮（B），并对其进行了体外抗菌活性测试，以评估其对金黄色葡萄球菌和大肠杆菌的抑制作用。此外，还对合成化合物进行了体外和计算机模拟的乙酰胆碱酯酶抑制活性测试。通过分子对接研究了羟基衍生物（B1-B6）的六个取代物的乙酰胆碱酯酶抑制活性。所有浓度的化合物均表现出剂量依赖性的抗菌活性。对接结果表明，所有化合物均比加兰他敏更稳定。其中，化合物 B1 在 AChE 和 BChE 酶中表现出最低的结合能。结果表明，香豆素衍生物具有作为潜在的抗菌和乙酰胆碱酯酶抑制剂的重要性。
