Tani J, Yamada Y, Oine T, Ochiai T, Ishida R, Inoue I
J Med Chem. 1979 Jan;22(1):95-9. doi: 10.1021/jm00187a021.
Some 2-(fluoromethyl) analogues of 2-methyl-3-aryl-4-(3H)-quinazolinones have been synthesized and screened for CNS activities. It was shown that the 2-(fluoromethyl) analogues possess in general more potent CNS depressant activities and less toxicities than their parent compounds. Of particular interest were the 2-(fluoromethyl) analogues (22, 24, and 31) of methaqualone and 6-aminomethaqualone. Compound 24 was more potent in CNS depressant activity and less toxic than methaqualone. Compound 31 exhbited potent central muscle relaxing activity and markedly reduced toxicity as compared with 6-aminomethaqualone.
已合成了一些2-甲基-3-芳基-4-(3H)-喹唑啉酮的2-(氟甲基)类似物，并对其进行了中枢神经系统活性筛选。结果表明，2-(氟甲基)类似物总体上比其母体化合物具有更强的中枢神经系统抑制活性和更低的毒性。特别令人感兴趣的是甲喹酮和6-氨基甲喹酮的2-(氟甲基)类似物(22、24和31)。化合物24的中枢神经系统抑制活性比甲喹酮更强，毒性更低。与6-氨基甲喹酮相比，化合物31表现出强大的中枢性肌肉松弛活性，且毒性明显降低。
