Conformational and Electronic Variations in 1,2‐ and 1,5a‐Cyclophellitols and their Impact on Retaining α‐Glucosidase Inhibition
作者:Tim P. Ofman、Jurriaan J. A. Heming、Alba Nin‐Hill、Florian Küllmer、Elisha Moran、Megan Bennett、Roy Steneker、Anne‐Mei Klein、Gijs Ruijgrok、Ken Kok、Zach W. B. Armstrong、Johannes M. F. G. Aerts、Gijsbert A. van der Marel、Carme Rovira、Gideon J. Davies、Marta Artola、Jeroen D. C. Codée、Herman S. Overkleeft
DOI:10.1002/chem.202400723
日期:2024.6.3
Twenty configurational and functional cyclophellitol analogues were synthesized and evaluated on their potency as retaining α-glucosidase inhibitors. The inhibitory properties of the focused library of compounds were determined on human α-glucosidases after which we mapped the conformationalfreeenergy landscapes of the most active compounds. Our results add to the growing list of covalent and competitive