%0 Journal Article
%T Phthalimide derivatives as a new class of papain‐like protease inhibitors in SARS‐CoV‐2
%V 358
%N 1
%P e2400714
%U https://onlinelibrary.wiley.com/doi/10.1002/ardp.202400714
%X Abstract 
             
              The severe acute respiratory syndrome coronavirus 2 (SARS‐CoV‐2) papain‐like cysteine protease (PLpro) represents one of only two essential cysteine proteases involved in the regulation of viral replication. It, therefore, qualifies as a promising therapeutic target for the development of antiviral agents. We identified a previously synthesized protease inhibitor, resulting from an earlier project, as a PLpro inhibitor and crafted a structure–activity relationship around the hit, leading to the more potent inhibitors ZHAWOC6941 ( 
              17h 
              ) and ZHAWOC25153 ( 
              17o 
              ) displaying IC 
              50 
              values of 8 and 7 µM, respectively. The two compounds represent a new class of PLpro inhibitors and, with single‐digit micromolar IC 
              50 
              values, are comparable to inhibitors found in the literature.
%G en
%J Archiv der Pharmazie
%A Fischer, Thomas
%A Frasson, David
%A Sievers, Martin
%A Riedl, Rainer
%D 01/2025