881816-26-8Relevant articles and documents
Thiazolinone heterocyclic compound, preparation method, medicinal composition and application thereof
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, (2019/01/09)
The invention provides a thiazolinone heterocyclic compound, a preparation method, a medicinal composition and an application thereof. The invention provides an application of the thiazolinone heterocyclic compound in preparation of an NLRP3 inflammasome inhibitor. The thiazolinone heterocyclic compound has a structure as a formula I or an isomer, a prodrug, or a pharmaceutically acceptable solvate or salt thereof.
Thiazolidinone CFTR inhibitors with improved water solubility identified by structure-activity analysis
Sonawane,Verkman
experimental part, p. 8187 - 8195 (2009/04/11)
The thiazolidinone 3-[(3-trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone (CFTRinh-172) inhibits cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel conductance with submicromolar affinity and blocks cholera toxin-induced intestinal fluid secretion. Fifty-eight CFTRinh-172 analogs were synthesized to identify CFTR inhibitors with improved water solubility, exploring modifications in its two phenyl rings, thiazolidinone core, and core-phenyl connectors. Greatest CFTR inhibition potency was found for 3-CF3 and polar group-substituted-phenyl rings, and a thiazolidinone core. Two compounds with ~1 μM CFTR inhibition potency and solubility >180 μM (>10-fold more than CFTRinh-172) were identified: Tetrazolo-172, containing 4-tetrazolophenyl in place of 4-carboxyphenyl, and Oxo-172, containing thiazolidinedione in place of the thiazolidinone core. These water soluble thiazolidinone analogs had low cellular toxicity. The improved water solubility of Tetrazolo- and Oxo-172 make them potential lead candidates for therapy of secretory diarrheas and polycystic kidney disease.