TY - JOUR
AU1 - Amador, Romain
AU2 - Delpal, Adrien
AU3 - Canard, Bruno
AU4 - Vasseur, Jean-Jacques
AU5 - Decroly, Etienne
AU6 - Debart, Françoise
AU7 - Clavé, Guillaume
AU8 - Smietana, Michael
AB - 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.
TI - Facile access to 4′-(N-acylsulfonamide) modified nucleosides and evaluation of their inhibitory activity against SARS-CoV-2 RNA cap N7-guanine-methyltransferase nsp14
JF - Organic and Biomolecular Chemistry
DO - 10.1039/d2ob01569b
DA - 2022-10-05
UR - https://www.deepdyve.com/lp/royal-society-of-chemistry/facile-access-to-4-n-acylsulfonamide-modified-nucleosides-and-d1AbaqvMFO
SP - 7582
EP - 7586
VL - 20
IS - 38
DP - DeepDyve
ER -