Dirlam J P, Czuba L J, Dominy B W, James R B, Pezzullo R M, Presslitz J E, Windisch W W
J Med Chem. 1979 Sep;22(9):1118-21. doi: 10.1021/jm00195a022.
A Free-Wilson analysis of the antibacterial activity found in a variety of quinoxaline 1,4-dioxides prepared and tested in these laboratories unexpectedly predicted that potent activity should be found in the case where the heterocyclic ring system was substituted with an acetyl group in the 2 position and a hydroxymethyl group in the 3 position (2). The synthesis and antibacterial activity of this compound, which was actually isolated in the hemiketal form (3), and of several of its derivatives are reported. 1-Hydroxy-1-methyl-1,3-dihydrofuro[3,4-b]quinoxaline 4,9-dioxide (3) possesses exceptional activity in vivo against Escherichia coli, Salmonella choleraesuis, and Pasteurella multocida.
对在这些实验室中制备并测试的多种喹喔啉-1,4-二氧化物的抗菌活性进行的Free-Wilson分析意外地预测，当杂环系统在2位被乙酰基取代且在3位被羟甲基取代时（2），应具有强效活性。报道了该化合物（实际上以半缩酮形式分离得到（3））及其几种衍生物的合成和抗菌活性。1-羟基-1-甲基-1,3-二氢呋喃并[3,4-b]喹喔啉-4,9-二氧化物（3）在体内对大肠杆菌、猪霍乱沙门氏菌和多杀巴斯德氏菌具有优异的活性。
