@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 {ZHAWOC}6941 ( 17h ) and {ZHAWOC}25153 ( 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.}, pages = {e2400714}, number = {1}, journaltitle = {Archiv der Pharmazie}, shortjournal = {Archiv der Pharmazie}, author = {Fischer, Thomas and Frasson, David and Sievers, Martin and Riedl, Rainer}, urldate = {2025-06-19}, date = {2025-01}, langid = {english}, }