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.
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| http://dx.doi.org/10.1080/14756366.2018.1471475 | DOI Listing |
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