Carta Antonio, Sanna Paolo, Loriga Mario, Setzu Maria Giovanna, La Colla Paolo, Loddo Roberta
Dipartimento Farmaco Chimico Tossicologico, Universitá di Sassari, Italy.
Farmaco. 2002 Jan;57(1):19-25. doi: 10.1016/s0014-827x(01)01153-3.
A new series of 3-isopropyl-, 3-trifluoromethyl- and 3-bromomethylquinoxaline-2-ones variously substituted on the benzo-moiety were synthesized and submitted to a preliminary in vitro evaluation for antibacterial, antifungal and anti-HIV activities. Furthermore, all compounds were also tested for cytotoxicity. Results of the screening showed that compound 10 exhibits moderate antimicrobial activity against Staphylococcus aureus (MIC = 33 microM), and that 25 and 26 showed interesting cytotoxicity versus mock-infected MT-4 cells. All the other compounds were inactive.
合成了一系列在苯并部分有不同取代基的3-异丙基-、3-三氟甲基-和3-溴甲基喹喔啉-2-酮，并对其进行了抗菌、抗真菌和抗HIV活性的初步体外评估。此外，还对所有化合物进行了细胞毒性测试。筛选结果表明，化合物10对金黄色葡萄球菌表现出中等抗菌活性（MIC = 33 microM），化合物25和26对模拟感染的MT-4细胞表现出有趣的细胞毒性。所有其他化合物均无活性。
