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Facile access to 4′-( N -acylsulfonamide) modified nucleosides and evaluation of their inhibitory activity against SARS-CoV-2 RNA cap N 7-guanine-methyltransferase nsp14

Abstract : N-Acylsulfonamides possess an additional carbonyl function compared to their sulfonamide analogues. Due to their unique physico-chemical properties, interest in molecules containing the N-acylsulfonamide moiety and especially nucleoside derivatives is growing in the field of medicinal chemistry. The recent renewal of interest in antiviral drugs derived from nucleosides containing a sulfonamide function has led us to evaluate the therapeutic potential of N-acylsulfonamide analogues. While these compounds are usually obtained by a difficult acylation of sulfonamides, we report here the easy and efficient synthesis of 20 4′-(N-acylsulfonamide) adenosine derivatives via the sulfo-click reaction. The target compounds were obtained from thioacid and sulfonyl azide synthons in excellent yields and were evaluated as potential inhibitors of the SARS-CoV-2 RNA cap N7-guanine-methyltransferase nsp14.
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https://hal-cnrs.archives-ouvertes.fr/hal-03801035
Contributor : Guillaume Clavé Connect in order to contact the contributor
Submitted on : Thursday, October 6, 2022 - 5:27:23 PM
Last modification on : Friday, November 18, 2022 - 3:55:46 AM

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Romain Amador, Adrien Delpal, Bruno Canard, Jean-Jacques Vasseur, Etienne Decroly, et al.. Facile access to 4′-( N -acylsulfonamide) modified nucleosides and evaluation of their inhibitory activity against SARS-CoV-2 RNA cap N 7-guanine-methyltransferase nsp14. Organic & Biomolecular Chemistry, 2022, 20 (38), pp.7582-7586. ⟨10.1039/d2ob01569b⟩. ⟨hal-03801035⟩

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