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Research Article

Antimicrobial, Anticancer and Immunomodulatory Potential of New Quinazolines Bearing Benzenesulfonamide Moiety

ORCID Icon, , ORCID Icon & ORCID Icon
Pages 275-290 | Received 07 Dec 2022, Accepted 24 Jan 2023, Published online: 09 Mar 2023
 

Abstract

Sulfonamides are privileged candidates with potent anti-methicillin-resistant Staphylococcus aureus (MRSA) activity and could replenish the MRSA antibiotic pipeline. The initial screening of a series of quinazolinone benzenesulfonamide derivatives 5–18 against multidrug-resistant bacterial and fungal strains revealed their potent activity. The promising compounds were conjugated with ZnONPs to study the effect of nanoparticle formation on the antimicrobial, cytotoxic and immunomodulatory activity. Compounds 5, 11, 16 and 18 revealed promising antimicrobial and cytotoxic activities with superior safety profiles and enhanced activity upon nanoformulation. The immunomodulatory potential of compounds 5, 11, 16 and 18 was assessed. Compounds 5 and 11 demonstrated an increase in spleen and thymus weight and boosted the activation of CD4+ and CD8+ T lymphocytes, confirming their promising antimicrobial, cytotoxic and immunomodulatory activity.

Graphical abstract

Supplementary data

To view the supplementary data that accompany this paper please visit the journal website at:www.tandfonline.com/doi/full/10.2217/epi-2016-0184

Acknowledgments

The authors appreciate the staff members of the gamma irradiation unit at the National Center for Radiation Research and Technology (NCRRT) for carrying out the irradiation process. AS Alqahtani is thankful to the Researchers Supporting Project (number RSP2023R132), King Saud University, Riyadh, Saudi Arabia.

Financial & competing interests disclosure

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending or royalties.

No writing assistance was utilized in the production of this manuscript.

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