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.

Evaluation of sulphonamide derivatives acting as inhibitors of human carbonic anhydrase isoforms I, II and Mycobacterium tuberculosis β-class enzyme Rv3273 / Wani, Tanvi V; Bua, Silvia; Khude, Pravin S; Chowdhary, Abdul H; Supuran, Claudiu T; Toraskar, Mrunmayee P. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - ELETTRONICO. - 33:(2018), pp. 0-0. [10.1080/14756366.2018.1471475]

Evaluation of sulphonamide derivatives acting as inhibitors of human carbonic anhydrase isoforms I, II and Mycobacterium tuberculosis β-class enzyme Rv3273

Bua, Silvia;Supuran, Claudiu T;
2018

Abstract

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.
2018
33
0
0
Wani, Tanvi V; Bua, Silvia; Khude, Pravin S; Chowdhary, Abdul H; Supuran, Claudiu T; Toraskar, Mrunmayee P
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Utilizza questo identificatore per citare o creare un link a questa risorsa: https://hdl.handle.net/2158/1308183
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