新型吡唑-磺胺类化合物的简便合成与表征及其对人碳酸酐酶同工酶的抑制作用。
Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes.
机构信息
Dumlupinar University, Art and Science Faculty, Department of Chemistry, 43100 Kütahya, Turkey.
出版信息
Bioorg Med Chem. 2013 Jan 1;21(1):21-7. doi: 10.1016/j.bmc.2012.11.012. Epub 2012 Nov 27.
In the current study, a series of pyrazole-sulfonamide derivatives (2-14) were synthesized, characterized, and the inhibition effects of the derivatives on human carbonic anhydrases (hCA I and hCA II) were investigated as in vitro. Structures of these sulfonamides were confirmed by FT-IR, (1)H NMR, (13)C NMR and LC-MS analysis. (1)H NMR and (13)C NMR revealed the tautomeric structures. hCA I and hCA II isozymes were purified from human erythrocytes and inhibitory effects of newly synthesized sulfonamides on esterase activities of these isoenzymes have been studied. The K(i) values of compounds were 0.062-1.278 μM for hCA I and 0.012-0.379 μM for hCA II. The inhibition effects of 7 for hCA I and 4 for hCA II isozymes were almost in nanomolar concentration range.
在当前的研究中，合成了一系列吡唑-磺酰胺衍生物（2-14），并对其进行了表征，同时作为体外研究，还考察了这些衍生物对人碳酸酐酶（hCA I 和 hCA II）的抑制作用。通过傅里叶变换红外光谱（FT-IR）、（1）H NMR、（13）C NMR 和 LC-MS 分析确定了这些磺酰胺的结构。（1）H NMR 和（13）C NMR 揭示了互变异构结构。从人红细胞中纯化了 hCA I 和 hCA II 同工酶，并研究了新合成的磺酰胺对这些同工酶酯酶活性的抑制作用。化合物对 hCA I 的 K(i)值为 0.062-1.278 μM，对 hCA II 的 K(i)值为 0.012-0.379 μM。7 对 hCA I 和 4 对 hCA II 同工酶的抑制作用几乎都在纳摩尔浓度范围内。
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