Ager I R, Harrison D R, Kennewell P D, Taylor J B
J Med Chem. 1977 Mar;20(3):379-86. doi: 10.1021/jm00213a013.
A number of derivatives of 2-methyl-3-(o-tolyl)-4(3H)-quinazolone bearing new substituents on the 2-methyl group have been synthesized. It was established that most substitutions at this position reduce or remove the CNS depressant activity of methaqualone. From the series prepared only the 2-fluoromethyl derivative or certain isothiouronium salts, which could be hydrolyzed in vivo to the 2-mercaptomethyl derivative, showed activity of the same magnitude as methaqualone.
已经合成了一系列在2-甲基上带有新取代基的2-甲基-3-（邻甲苯基）-4（3H）-喹唑酮衍生物。已确定该位置的大多数取代会降低或消除甲喹酮的中枢神经系统抑制活性。在所制备的系列中，只有2-氟甲基衍生物或某些异硫脲盐（可在体内水解为2-巯基甲基衍生物）显示出与甲喹酮相同程度的活性。
