He, Cheng-yan’s team published research in Chemical Research in Chinese Universities in 20 | CAS: 307510-92-5

Chemical Research in Chinese Universities 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 C18H10F3NO3S2, Category: thiazolidine.

He, Cheng-yan published the artcileSynthesis and characterization of a small molecule CFTR chloride channel inhibitor, Category: thiazolidine, the publication is Chemical Research in Chinese Universities (2004), 20(3), 334-337, database is CAplus.

A thiazolidinone CFTR inhibitor (CFTRinh-172) was synthesized by a three-step procedure with trifluoromethylaniline as the starting material. The synthesized CFTR inhibitor was characterized structurally by 1H-NMR and functionally in a CFTR-expressing cell line FRT/hCFTR/EYFP-H148Q by both fluorescent and electrophysiol. methods. A large amount (100 g) of high-quality small mol. thiazolidinone CFTR chloride channel inhibitor, CFTRinh-172, can be produced with this simple three-step synthetic procedure. The structure of the final product 2-thioxo-3-(3-trifluoromethylphenyl)-5-[4-carboxyphenyl-methylene]-4-thiazolidinone was confirmed by 1H NMR. The overall yield was 58% with a purity over 99% as analyzed by HPLC. The synthesized CFTRinh-172 specifically inhibited CFTR chloride channel function in a cell-based fluorescence assay (Kd≈1.5 μmol/L) and in a Ussing chamber-based short-circuit current assay (Kd≈0.2 μmol/L), indicating better quality than that of the com. combinatorial compound The synthesized inhibitor is nontoxic to cultured cells at a high concentration and to mouse at a high dose. The synthetic procedure developed here can be used to produce a large amount of the high-quality CFTRinh-172 suitable for antidiarrheal studies and for creation of cystic fibrosis models in large animals. The procedure can be used to synthesize radiolabeled CFTRinh-172 for in vivo pharmacokinetics studies.

Chemical Research in Chinese Universities 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 C18H10F3NO3S2, Category: thiazolidine.

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