A green synthesis of N-acylsulfonamides was developed. Some of these compounds showed in vivo anti-inflammatory activity that surpasses the efficacy of diclofenac. These results are in good agreement with the in silico study.
A method has been developed for preparing N-acylsulfonamides via a metal triflimide-catalyzed acylation of sulfonamides and transacylation of N-acylsulfonamides.
A one-pot method has been developed to prepare N-sulfonylamidines from N-acylsulfonamides via a metal triflate-catalyzed nonhydrolytic deacylation followed by interception of the newly formed sulfonamide with N,N-dimethylformamide dimethyl acetal.
Replacement of a key carboxylic acid in a dual MCL-1/BCL-xL inhibitor with bioisosteres was successful, and resulted in the discovery of an acylsulfonamide-derived compound (7d) with the greatest anti-leukemic activity of the entire series.
Modified oligonucleotides incorporating NAC linkages were synthesized and evaluated to improve nuclease resistance and modulate biological properties.