Facile synthetic approach towards vasorelaxant active 4-hydroxyquinazoline-4-carboxamides

Marian N. Aziz, Siva S. Panda, Elsayed M. Shalaby, Nehmedo G. Fawzy, Adel S. Girgis

Research output: Contribution to journalArticle

2 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)28534-28540
Number of pages7
JournalRSC Advances
Volume9
Issue number49
DOIs
StatePublished - Jan 1 2019

ASJC Scopus subject areas

  • Chemistry(all)
  • Chemical Engineering(all)

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