Synthesis and characterization of some new pyrazolines and their inhibitory potencies against carbonic anhydrases,Archiv der Pharmazie

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Synthesis and characterization of some new pyrazolines and their inhibitory potencies against carbonic anhydrases
Archiv der Pharmazie ( IF 4.3 ) Pub Date : 2020-01-10 , DOI: 10.1002/ardp.201900292
Gonca Çelik ₁ , Tayfun Arslan ₂ , Murat Şentürk ₃ , Deniz Ekinci ₄

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The inhibition of the two human cytosolic carbonic anhydrase (hCA; EC 4.2.1.1) isozymes I and II with some new pyrazoline derivatives was investigated for the first time. The structures of the newly synthesized pyrazoline derivatives were characterized by Fourier transform‐infrared spectroscopy, 1H‐/13C‐nuclear magnetic resonance, and mass spectrometry, and elemental analysis. Compounds 1–6 showed Ki values in the range of 16.4–205.9 nM for hCA I and of 6.08–93.21 nM against hCA II. These hydroxyl and amino group‐containing compounds generally were competitive inhibitors. The compounds investigated here showed effective hCA I and II inhibitory effects, in the same range as the clinically used acetazolamide, and might be used as leads for generating enzyme inhibitors, possibly targeting other CA isoforms that have not yet been assayed for their interactions with such agents.

中文翻译：

一些新型吡唑啉类化合物的合成和表征及其对碳酸酐酶的抑制作用

首次研究了一些新的吡唑啉衍生物对两种人胞质碳酸酐酶 (hCA; EC 4.2.1.1) 同工酶 I 和 II 的抑制作用。新合成的吡唑啉衍生物的结构通过傅里叶变换红外光谱、1H-/13C-核磁共振、质谱和元素分析进行表征。化合物 1-6 对 hCA I 的 Ki 值在 16.4-205.9 nM 的范围内，对 hCA II 的 Ki 值在 6.08-93.21 nM 的范围内。这些含羟基和氨基的化合物通常是竞争性抑制剂。这里研究的化合物显示出有效的 hCA I 和 II 抑制作用，与临床使用的乙酰唑胺范围相同，并且可能用作产生酶抑制剂的先导物，

更新日期：2020-01-10

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