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Synthesis of some quinazolin-4-one derivatives carrying ibuprofenyl moiety and their antiinflammatory activity | Abstract

Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

ISSN: 0975-413X
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Abstract

Synthesis of some quinazolin-4-one derivatives carrying ibuprofenyl moiety and their antiinflammatory activity

Author(s): Ayman M. F. Elgohary1,2, Mohamed M. Hassan3,4, and Mohamed Abass4,*

A new series of antiinflammatory active Ibuprofen derivatives comprises quinazolinone moiety was synthesized. Ibuprofen was converted into its acid chloride 1 and reacted with anthranilic acid to give the anilide 2. The anilide 2 was refluxed with acetic anhydride to form benzoxazinone 3. The later on reaction with nitrogen nucleophile such as hydrazine hydrate, gave 3-aminoquinazolinone 4. The compound 4 was used as key starting material to synthesize twelve quinazolinone derivatives 5, 6, 7a-c, 8a-c, 9a-c, and 10. The structures of the synthesized compounds have been established on the basis of spectral and analytical data. All the synthesized compounds have been estimated as anti-inflammatory with minimal ulceroginc effect.


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