ArticleBioorganic & medicinal chemistry2008
Thiazolidinone CFTR inhibitors with improved water solubility identified by structure-activity analysis.
Article in Bioorganic & medicinal chemistry, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
23 citing papers in PubMed.
- Epithelial plasma membrane transporters as drug targets.Physiological reviews · 2026Review
- Structure of CFTR bound to (R)-BPO-27 unveils a pore-blockage mechanism.Nature communications · 2025Article
- Allosteric inhibition of CFTR gating by CFTRinh-172 binding in the pore.Nature communications · 2024Article
- Recommended Tool Compounds for Modifying the Cystic Fibrosis Transmembrane Conductance Regulator Channel Variants.ACS pharmacology & translational science · 2024Review
- Structural basis for CFTR inhibition by CFTRProceedings of the National Academy of Sciences of the United States of America · 2024Article
- The mechanism of NLRP3 inflammasome activation and its pharmacological inhibitors.Frontiers in immunology · 2022Review
- Chloride transport modulators as drug candidates.American journal of physiology. Cell physiology · 2021Review
- Promise of the NLRP3 Inflammasome Inhibitors in In Vivo Disease Models.Molecules (Basel, Switzerland) · 2021Review
- Pharmacological Inhibitors of the NLRP3 Inflammasome.Frontiers in immunology · 2019Review
- Identification of a selective and direct NLRP3 inhibitor to treat inflammatory disorders.The Journal of experimental medicine · 2017Article
- CFTR pharmacology.Cellular and molecular life sciences : CMLS · 2017Review
- Pharmacological modulation of the AKT/microRNA-199a-5p/CAV1 pathway ameliorates cystic fibrosis lung hyper-inflammation.Nature communications · 2015Article
- Discovery and development of antisecretory drugs for treating diarrheal diseases.Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association · 2014Review
- Chloride channel-targeted therapy for secretory diarrheas.Current opinion in pharmacology · 2013Review
- Reduced caveolin-1 promotes hyperinflammation due to abnormal heme oxygenase-1 localization in lipopolysaccharide-challenged macrophages with dysfunctional cystic fibrosis transmembrane conductance regulator.Journal of immunology (Baltimore, Md. : 1950) · 2013Article
- ABSOLUTE CONFIGURATION AND BIOLOGICAL PROPERTIES OF ENANTIOMERS OF CFTR INHIBITOR BPO-27.ACS medicinal chemistry letters · 2013Article
- CFTR inhibitors.Current pharmaceutical design · 2013Review
- Potent, metabolically stable benzopyrimido-pyrrolo-oxazine-dione (BPO) CFTR inhibitors for polycystic kidney disease.Journal of medicinal chemistry · 2011Article
- Role of CFTR expressed by neutrophils in modulating acute lung inflammation and injury in mice.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2011Article
- Abnormal trafficking and degradation of TLR4 underlie the elevated inflammatory response in cystic fibrosis.Journal of immunology (Baltimore, Md. : 1950) · 2011Article
Corrections and comments
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Authors and funding
2 authors.
Funding
Abstract
The thiazolidinone 3-[(3-trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone (CFTR(inh)-172) inhibits cystic fibrosis transmembrane conductance regulator (CFTR) chloride channel conductance with submicromolar affinity and blocks cholera toxin-induced intestinal fluid secretion. Fifty-eight CFTR(inh)-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-CF(3) and polar group-substituted-phenyl rings, and a thiazolidinone core. Two compounds with approximately 1muM CFTR inhibition potency and solubility >180 microM (>10-fold more than CFTR(inh)-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.
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