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A thiazolidinone CFTR inhibitor (CFTRinh-72) was synthesized by a three-step procedure with tri-fluromethylaniline as the starting material. The synthesized CFTR inhibitor was characterized structurally bymeans of ^1H NMR and functionally in a CFTR-expressing cell line FRT/hCFTR/EYFP-H148Q by both fluo-rescent and electrophysiological methods. A large amount(100g) of high-quality small molecule thiazolidi-none CFTR chloride channel inhibitor, CFTRinh-72, can be produced with this simple three-step synthetic pro-cedure. The structure of the final product 2-thioxo-3-(3-trifluromethylphenyl )-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-72 specifically inhibited CFTR chloride channel function in acell-based fluorescence assay(Kd≈1.5μmol/L) and in a Ussing chamber-based short-circuit current assay(Kd≈0. 2μmol/L), indicating better quality than that of the commercial combinatorial compound. The syn-thesized inhibitor is nontoxic to cultured cells at a high concentration and to mouse at a high dose. The syn-thetic procedure developed here can be used to produce a large amount of the high-quality CFTRinh-72 suitablefor antidiarrheal studies and for creation of cystic fibrosis models in large animals. The procedure can be usedto synthesize radiolabled CFTRinh-72 for in νiνo pharmacokinetics studies. 相似文献
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SHI Lin-lin XU Li-na HOU Shu-guang LIN Sen YANG Hong MA Tong-hui 《高等学校化学研究》2006,22(3):312-314
Introduction Aloe,cascaraandsennaarewidelyusedasall purposelaxativemedicine.Itisgenerallyregardedthat thecatharticingredientsofaloe,cascaraandsennaare anthraquinoneandtheirderivatives[1].Ithasbeenwell definedthattheincreasedleakingofplasmaintointesti nall… 相似文献
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