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Chemical Studies on Some Chromone Derivatives with Anticipated Pharmaceutical Applications: Thesis Abstract

Authors :
El-Sayed I. El-Desoky
Eman M. Keshk
Aya Atef El-Sawi
A. H. Abdel-Rahman
Source :
International Journal of Cancer and Biomedical Research.
Publication Year :
2021
Publisher :
Egypts Presidential Specialized Council for Education and Scientific Research, 2021.

Abstract

The present study reports a convenient protocol for the design and synthesis of new heterocyclic compounds incorporating 1- hydroxy-naphthyl and new angular chromones bearing allylnaphthyl fragments. The versatile precursor 2-acetyl-4- allyl-1-hydroxy naphthalene was subjected to Claisen-Schmidt condensation but The precursor 6-allyl-3-formyl-4H-benzo[h]chromone was prepared via Vilsmeier–Haack reaction of 4-allyl-1- hydroxy-2-acetonaphthone.Some new compounds are considered as promising leads with dual biological activity as antibacterial and antioxidant. The isoalloxazine ring of the cofactor FAD is essential to the recognition of the compound that has proper antioxidant activity. Benzocoumarin ring is essential for the recognition of the amino acid residues. Allyl chain improves the p stacking interaction while the n-propyl chain attenuates the overall interaction. Naphthyl ring needs to be substituted with a short bridge to avid the ring extended away from the pocket.The antimicrobial and antiquorum-sensing activities of the newly synthesized compounds showed that many compounds have good and promising activities in comparison with the reference drugs. Computational prediction of pharmacokinetics, drug-likeness properties, biological activity, and molecular docking suggested that formyl chromone and tetracarbonyl may be potent antimicrobial drugs.

Details

ISSN :
26822628
Database :
OpenAIRE
Journal :
International Journal of Cancer and Biomedical Research
Accession number :
edsair.doi...........f00c11aa063879b378faaea07cebe269
Full Text :
https://doi.org/10.21608/jcbr.2021.60308.1142