期刊
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
卷 33, 期 1, 页码 962-971出版社
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2018.1471475
关键词
Carbonic anhydrase; sulphonamide; human isoforms I and II; Mycobacterium tuberculosis
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-1- and C-13-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 beta-CA encoded by the gene Rv3273 (mtCA 3) inhibition activity was investigated with the synthesised compounds which showed promising inhibition. The K(I)s were in the range of 54.6nM-1.8 mu M against hCA I, in the range of 32.1 nM-5.5 mu M against hCA II and of 127 nM-2.12 mu M against mtCA 3.
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