Syntheses and Pharmacological Activities of 2-Heterocyclic Substituted 4(3H)-Quinazolinone Derivatives

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概要

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• The preparation of series of 2-pyridyl-4(3H)-quinazolinones is described. Some of them showed a hypnotic action in mice when given orally. Studies on the structure-activity relationship demonstrated that 2-pyridyl, 3-pyridyl, and 4-pyridyl substitution at 2 position of quinazolinone ring, and o-, m-, and p-substitution of the aromatic ring at 3 position are suitable for manifestation of hypnotic activity. The order of potency of activities produced by the difference in the position of substitution of substituents at 2 and 3 position decreased in the order of 4-pyridyl, o-tolyl>3-pyridyl, o-tolyl>2-pyridyl, o-tolyl. The anthranilates of these 4(3H)-quinazolinones were inactive. A maximum hypnotic effect accompanied with other potent pharmacological properties was observed in 2-(4-pyridyl)-3-o-tolyl-4(3H)-quinazolinone (14), the potency of which was equal to or stronger than Methaqualone in mice.

• 社団法人日本薬学会の論文
• 1972-12-25

著者

• 市川 正孝

  福山大学薬学部

• 市川 正孝

  Faculty Of Pharmaceutical Sciences Kumamoto Univerisity

• 久野 拓造

  Faculty Of Pharmaceutical Sciences Kumamoto University

• 鬼頭 剛

  Faculty Of Pharmaceutical Sciences Kumamoto University

• 久野 拓三

  熊本大学薬学部

• 西 知行

  Faculty of Pharmaceutical Sciences, Kumamoto University

• 西 知行

  熊本大学薬学部

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