ArticleMedicinal chemistry (Shariqah (United Arab Emirates))2024
Substituted 4H-3,1-benzoxazine-4-one Derivatives as Inhibitors of Cathepsin G.
Article in Medicinal chemistry (Shariqah (United Arab Emirates)), 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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2 authors at 2 institutions in 1 country.
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Abstract
backgroundCathepsin G (CatG) is a cationic serine protease with a wide substrate specificity. CatG has been reported to play a role in several pathologies, including rheumatoid arthritis, ischemic reperfusion injury, acute respiratory distress syndrome, and cystic fibrosis, among others.
objectiveWe aim to develop a new class of CatG inhibitors and evaluate their potency and selectivity against a series of serine proteases.
methodsWe exploited chemical synthesis as well as chromogenic substrate hydrolysis assays to construct and evaluate the new inhibitors.
resultsIn this communication, we report on a new class of CatG inhibitors of 4H-3,1-benzoxazin- 4-one derivatives. We constructed a small library of seven substituted 4H-3,1-benzoxazin-4-one derivatives and identified their inhibition potential against CatG. Five molecules were identified as CatG inhibitors with values of 0.84-5.5 μM. Inhibitor 2 was the most potent, with an IC
conclusionThus, we propose this inhibitor as a lead molecule to guide subsequent efforts to develop clinically relevant potent and selective CatG inhibitors for use as anti-inflammatory agents.
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