STUDIES ON BIOLOGICALLY-ACTIVE HALOGENATED COMPOUNDS .1. SYNTHESIS AND CENTRAL NERVOUS-SYSTEM DEPRESSANT ACTIVITY OF 2-(FLUOROMETHYL)-3-ARYL-4(3H)-QUINAZOLINONE DERIVATIVES

被引：99

作者：

TANI, J ^{[1
]}

YAMADA, Y ^{[1
]}

OINE, T ^{[1
]}

OCHIAI, T ^{[1
]}

ISHIDA, R ^{[1
]}

INOUE, I ^{[1
]}

机构：

[1] TANABE SEIYAKU CO LTD,RES LABS,16-89 KASHIMA 3 CHOME,YODOGAWA KU,OSAKA 532,JAPAN

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1979年 / 22卷 / 01期

关键词：

D O I：

10.1021/jm00187a021

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

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 exhibited potent central muscle relaxing activity and markedly-reduced toxicity as compared with 6-aminomethaqualone. © 1979, American Chemical Society. All rights reserved.

引用

页码：95 / 99

页数：5

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