Literature DB >> 845871

Synthesis and central nervous system activity of quinazolones related to 2-methyl-3-(o-tolyl)-4(3H)-quinazolone (methaqualone).

I R Ager, D R Harrison, P D Kennewell, J B Taylor.   

Abstract

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.

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Year:  1977        PMID: 845871     DOI: 10.1021/jm00213a013

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  3 in total

1.  Synthesis of benzoxazinone derivatives: a new route to 2 (N phthaloylmethyl)-4H-3,1-benzoxazin-4-one.

Authors:  Mehdi Shariat; Sohrab Abdollahi
Journal:  Molecules       Date:  2004-07-31       Impact factor: 4.411

2.  Ru(II)/Ir(III)-Catalyzed C-H Bond Activation/Annulation of Cyclic Amides with 1,3-Diketone-2-diazo Compounds: Facile Access to 8H-Isoquinolino[1,2-b]quinazolin-8-ones and Phthalazino[2,3-a]cinnoline-8,13-diones.

Authors:  Panyuan Cai; Enshen Zhang; Yinsong Wu; Taibei Fang; Qianqian Li; Chen Yang; Jian Wang; Yongjia Shang
Journal:  ACS Omega       Date:  2018-11-01

3.  Synthesis and anticonvulsant activity of some quinazolin-4-(3H)-one derivatives.

Authors:  Hanan Georgey; Nagwa Abdel-Gawad; Safinaz Abbas
Journal:  Molecules       Date:  2008       Impact factor: 4.411

  3 in total

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