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Updated: Jan 8, 2026

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Synthesis and Biological Activity of Some Novel Quinolinones Derived from
Fatma Youssef1, Mostafa Ismail1, Mohammed Abass1
1Ain Shams University, Cairo, Egypt.
Abstract:
The reactivity of 1-ethyl-1,2-dihydro-4-hydroxy-2-oxoquinoline-3-carbaldehyde (1) towards some diaza-nucleophiles has been investigated, under various reaction conditions. 1-Ethyl-1,2-dihydro-4-hydroxy-2-oxoquinoline-3-carbaldehyde (1) was reacted with hydrazine, phenylhydrazine, 2,4-dinitrophenylhydrazine, acid hydrazides, semicarbazide, thiosemicarbazides, thiocarbohydrazide, ortho-phenylenediamine and ortho-aminophenol. It was found that solvents used in these reactions impacted product selectivity. Accordingly, these reactions led to various open-chain and/or cyclic derivatives of quinolinone. The structure of the new compounds was determined using spectroscopic techniques and elemental analyses. All products were screened in vitro to determine their antimicrobial, antioxidant and antitumor activities. Compounds 2a and 2c are the most active compounds against bacterial and fungal strains. While the most effective compounds against breast cancer (MCF-7) are compounds 2a and 8a.
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