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Updated: Sep 24, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides
Marian N Aziz1, Siva S Panda2, ElSayed M Shalaby3
1Department of Pesticide Chemistry, National Research Centre Dokki Giza 12622 Egypt girgisas10@yahoo.com.
Abstract:
A Facile synthetic approach is reported towards 4-hydroxyquinazoline-4-carboxamides 13a-i through ring expansion of 2,3-dioxoindoline-1-carboxamides 10a-c during secondary amine 11a-d nucleophilic reaction. Single crystal X-ray studies of 10c and 13d support the structures. Some of the synthesized quinazolinecarboxamides 13 show promising vasorelaxant properties with potency higher than that of Doxazosin through the pre-contracted (norepinephrine hydrochloride) rat aorta standard bioassay. Good molecular models (2D-QSAR, pharmacophore) describe the biological observations.
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