Triazenes as inhibitors of HIV-1 and HCoV-OC43: A structure-activity relationship study

Mérindol, N., Hashemian, S. M., Sokhna, S., Girard, M.-P., Presset, M., Seck, I., Ba, L. A., Ka, S., Ndoye, S. F., Samb, I., Le Gall, E., Berthoux, L., Seck, M. et Desgagné-Penix, I. (2025). Triazenes as inhibitors of HIV-1 and HCoV-OC43: A structure-activity relationship study. European Journal of Medicinal Chemistry Reports, 15 . Article 100288. ISSN 2772-4174 DOI 10.1016/j.ejmcr.2025.100288

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Résumé

Abstract
Triazenes, or amino-substituted diazenes, are organic compounds containing three contiguous nitrogen atoms, that have potent biological activities. We previously demonstrated that triazenes, particularly those substituted with a phenyl or 3-pyridyl ring at the 1-position and a 2-pyridyl ring at the 3-position, exhibit anti-DENV properties. Here, we evaluated the antiviral activity against a betacoronavirus (HCoV-OC43) and a lentivirus (HIV-1). 1-(4-trifluoromethylphenyl)-2-imidazole-1-yldiazene (21) exhibited broad-spectrum activity (EC50 = 6.6–6.8 μM) but was cytotoxic to THP-1 cells. Pyridyl triazenes (14, 15) were the most potent against HCoV-OC43, while 1-(4-methoxyphenyl)-2-morpholin-4-yldiazene (6) and 1-(4-methoxyphenyl)3-(-6-methylpyridin-2-yl)triazene (10) inhibited HIV-1 the most. Structure–activity relationship analysis, supported by molecular docking, indicated that para-methoxy groups favored interactions with viral enzyme binding pockets, enhancing antiviral potency, while meta and para-trifluoromethyl groups were associated with reduced activity and increased cytotoxicity. These findings support the further development of triazenes as antiviral scaffolds.

Type de document:	Article
Mots-clés libres:	Diazene Therapeutic compounds Antiviral Nitrogen Functional groups Lentiviridae Coronaviridae Docking
Date de dépôt:	07 janv. 2026 16:43
Dernière modification:	07 janv. 2026 16:43
Version du document déposé:	Version officielle de l'éditeur
URI:	https://depot-e.uqtr.ca/id/eprint/12517

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