N-酰基磺胺类化合物强烈抑制人类碳酸酐酶同工酶I和II。
N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II.
作者信息
Yıldırım Alper, Atmaca Ufuk, Keskin Ali, Topal Meryem, Çelik Murat, Gülçin İlhami, Supuran Claudiu T
机构信息
Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey.
Gumushane University, Vocational School of Health Services, Department of Medical Services and Techniques, Gumushane, Turkey.
出版信息
Bioorg Med Chem. 2015 May 15;23(10):2598-605. doi: 10.1016/j.bmc.2014.12.054. Epub 2015 Mar 20.
Sulfonamides represent a significant class of biologically active compounds that inhibit carbonic anhydrase (CA, EC.: 4.2.1.1) isoenzymes involved in different pathological and physiological events. Sulfonamide CA inhibitors are used therapeutically as diuretic, antiglaucoma, antiobesity and anticancer agents. A series of new sulfonamides were synthesized using imides and tosyl chloride as starting materials. These N-acylsulfonamides efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I, and II (hCA I, and II), with nanomolar range inhibition constants ranging between 36.4 ± 6.0-254.6 ± 18.0 and 58.3 ± 0.6-273.3 ± 2.5 nM, respectively.
磺胺类药物是一类重要的生物活性化合物，可抑制参与不同病理和生理过程的碳酸酐酶（CA，EC：4.2.1.1）同工酶。磺胺类碳酸酐酶抑制剂在治疗上用作利尿剂、抗青光眼药、减肥药和抗癌药。以酰亚胺和对甲苯磺酰氯为起始原料合成了一系列新型磺胺类药物。这些N-酰基磺胺有效地抑制了胞质型人碳酸酐酶同工酶I和II（hCA I和II），抑制常数在纳摩尔范围内，分别为36.4±6.0 - 254.6±18.0和58.3±0.6 - 273.3±2.5 nM。
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