Sonawane, N. D.’s team published research in Bioorganic & Medicinal Chemistry in 16 | CAS: 307510-92-5

Bioorganic & Medicinal Chemistry published new progress about 307510-92-5. 307510-92-5 belongs to thiazolidine, auxiliary class Membrane Transporter/Ion Channel,CFTR, name is 4-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acid, and the molecular formula is C19H36BNO2Si, HPLC of Formula: 307510-92-5.

Sonawane, N. D. published the artcileThiazolidinone CFTR inhibitors with improved water solubility identified by structure-activity analysis, HPLC of Formula: 307510-92-5, the publication is Bioorganic & Medicinal Chemistry (2008), 16(17), 8187-8195, database is CAplus and MEDLINE.

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 Ph rings, thiazolidinone core, and core-Ph connectors. Greatest CFTR inhibition potency was found for 3-CF3 and polar group-substituted-Ph 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.

Bioorganic & Medicinal Chemistry published new progress about 307510-92-5. 307510-92-5 belongs to thiazolidine, auxiliary class Membrane Transporter/Ion Channel,CFTR, name is 4-((4-Oxo-2-thioxo-3-(3-(trifluoromethyl)phenyl)thiazolidin-5-ylidene)methyl)benzoic acid, and the molecular formula is C19H36BNO2Si, HPLC of Formula: 307510-92-5.

Referemce:
https://en.wikipedia.org/wiki/Thiazolidine,
Thiazolidine – ScienceDirect.com