评价作为人碳酸酐酶同工酶 I、II 和结核分枝杆菌β 类酶 Rv3273 抑制剂的磺胺衍生物。
Evaluation of sulphonamide derivatives acting as inhibitors of human carbonic anhydrase isoforms I, II and Mycobacterium tuberculosis β-class enzyme Rv3273.
机构信息
a Department of Pharmaceutical Chemistry , Bharati Vidyapeeth's College of Pharmacy , Navi Mumbai , India.
b NEUROFARBA Department, Sezione di Scienze Farmaceutiche , Università degli Studi di Firenze , Sesto Fiorentino , Florence , Italy.
出版信息
J Enzyme Inhib Med Chem. 2018 Dec;33(1):962-971. doi: 10.1080/14756366.2018.1471475.
A series of novel sulphonamide derivatives was obtained from sulphanilamide which was N4-alkylated with ethyl bromoacetate followed by reaction with hydrazine hydrate. The hydrazide obtained was further reacted with various aromatic aldehydes. The novel sulphonamides were characterised by infrared, mass spectrometry, H- and C-NMR and purity was determined by high-performance liquid chromatography (HPLC). Human (h) carbonic anhydrase (CA, EC 4.2.1.1) isoforms hCA I and II and Mycobacterium tuberculosis β-CA encoded by the gene Rv3273 (mtCA 3) inhibition activity was investigated with the synthesised compounds which showed promising inhibition. The Ks were in the range of 54.6 nM-1.8 µM against hCA I, in the range of 32.1 nM-5.5 µM against hCA II and of 127 nM-2.12 µM against mtCA 3.
一系列新型磺胺衍生物是由磺胺经溴乙酸乙酯 N4-烷基化，然后与水合肼反应得到的。得到的酰肼进一步与各种芳香醛反应。新型磺胺通过红外光谱、质谱、H-和 C-NMR 进行了表征，并通过高效液相色谱 (HPLC) 确定了纯度。用合成的化合物研究了人碳酸酐酶 (CA，EC 4.2.1.1) 同工酶 hCA I 和 II 以及由基因 Rv3273 编码的结核分枝杆菌 β-CA（mtCA 3）的抑制活性，结果显示出有希望的抑制作用。对 hCA I 的抑制 Ks 值在 54.6 nM-1.8 μM 范围内，对 hCA II 的抑制 Ks 值在 32.1 nM-5.5 μM 范围内，对 mtCA 3 的抑制 Ks 值在 127 nM-2.12 μM 范围内。
Zotero 插件