@article{fischer_phthalimide_2025, title = {Phthalimide derivatives as a new class of papain‐like protease inhibitors in {SARS}‐{CoV}‐2}, volume = {358}, issn = {0365-6233, 1521-4184}, url = {https://onlinelibrary.wiley.com/doi/10.1002/ardp.202400714}, doi = {10.1002/ardp.202400714}, abstract = {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.}, language = {en}, number = {1}, urldate = {2025-06-19}, journal = {Archiv der Pharmazie}, author = {Fischer, Thomas and Frasson, David and Sievers, Martin and Riedl, Rainer}, month = jan, year = {2025}, pages = {e2400714}, }