2-(dialkylamino)-4H-1-benzopyran-4-one derivatives modify chloride conductance in CFTR expressing cells.
Some 2-(diethylamino)-7-hydroxy-4H-1-benzopyran-4-one derivatives, potentially useful as activators of the cystic fibrosis transmembrane conductance regulator (CFTR), were prepared. The synthesized compounds were tested, together with others 2-(dialkylamino)-7-hydroxybenzopyran-4-one derivatives, by measuring their capacity to modify the kinetics of iodide influx in Fisher rat thyroid cells expressing wild type CFTR and the halide-sensitive yellow fluorescent protein. Among the tested compounds the dinitrile derivatives 8 and 9 are endowed with an activity comparable to the reference compound apigenin.
D000818:Animals; D001578:Benzopyrans / Q000737:chemistry / Q000494:pharmacology*; D002712:Chlorides / Q000378:metabolism*; D019005:Cystic Fibrosis Transmembrane Conductance Regulator / Q000819:agonists / Q000378:metabolism*; D015195:Drug Design; D007454:Iodides / Q000378:metabolism; D051381:Rats; D011916:Rats, Inbred F344; D013329:Structure-Activity Relationship; D013961:Thyroid Gland / Q000166:cytology / Q000378:metabolism
D001578:Benzopyrans; D002712:Chlorides; D007454:Iodides; D019005:Cystic Fibrosis Transmembrane Conductance Regulator