氟代磺酰胺衍生物的合成及对碳酸酐酶抑制作用的研究。
Synthesis and investigation of inhibition effect of fluorinated sulfonamide derivatives on carbonic anhydrase.
机构信息
Institut des Biomolécules Max Mousseron UMR CNRS 5247 Université de Montpellier I et de Montpellier II, CC1706, Place Eugène Bataillon 34095 Montpellier cedex 05, France.
出版信息
Eur J Med Chem. 2010 Mar;45(3):1225-9. doi: 10.1016/j.ejmech.2009.11.052. Epub 2009 Dec 5.
Series of perfluoroalkanesulfonamides 1, sodium salt of perfluoroalkanesulfonamides 2 and polyfluoroalkanesulfonamides 3 derivatives were synthesized and characterized by (1)H NMR, (13)C NMR, (19)F NMR, IR and HRMS. Inhibition effects of these compounds on bovine carbonic anhydrase (bCA) and human carbonic anhydrase isoenzyme II (hCA) have been investigated. Comparing IC(50) values of the synthesized molecules 1, 2 and 3, it has been found that compound 2b is a more potent inhibitor than acetazolamide on hCA. Moreover 2b does not present cellular toxicity on sheep red globules.
一系列全氟烷磺酰胺 1、全氟烷磺酰胺钠盐 2 和多氟烷磺酰胺 3 的衍生物被合成并通过 (1)H NMR、(13)C NMR、(19)F NMR、IR 和 HRMS 进行了表征。这些化合物对牛碳酸酐酶 (bCA) 和人碳酸酐酶同工酶 II (hCA) 的抑制作用进行了研究。比较合成分子 1、2 和 3 的 IC(50) 值，发现化合物 2b 对 hCA 的抑制作用比乙酰唑胺更强。此外，2b 在绵羊红细胞上没有表现出细胞毒性。
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