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Microwave-assisted synthesis and bioevaluation of new sulfonamides.

ABSTRACT: In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13C NMR and HRMS. Cytotoxic activities and inhibitory effects on carbonic anhydrase I and II isoenzymes of the compounds were investigated. The compounds 9 (PSE?=?4.2), 12 (PSE?=?4.1) and 13 (PSE?=?3.9) with the highest potency selectivity expression (PSE) values in cytotoxicity experiments and the compounds 13 (Ki?=?3.73?±?0.91?nM toward hCA I) and 14 (Ki?=?3.85?±?0.57?nM toward hCA II) with the lowest Ki values in CA inhibition studies can be considered as leader compounds for further studies.

SUBMITTER: Gul HI

PROVIDER: S-EPMC6009867 | biostudies-literature | 2017 Dec

REPOSITORIES: biostudies-literature

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Microwave-assisted synthesis and bioevaluation of new sulfonamides.

Gul Halise Inci HI Yamali Cem C Yesilyurt Fatma F Sakagami Hiroshi H Kucukoglu Kaan K Gulcin Ilhami I Gul Mustafa M Supuran Claudiu T CT

Journal of enzyme inhibition and medicinal chemistry 20171201 1

In this study, 4-[5-(4-hydroxyphenyl)-3-aryl-4,5-dihydro-1H-pyrazol-1-yl]benzenesulfonamide derivatives (8-14) were synthesized for the first time by microwave irradiation and their chemical structures were confirmed by <sup>1</sup>H NMR, <sup>13</sup>C NMR and HRMS. Cytotoxic activities and inhibitory effects on carbonic anhydrase I and II isoenzymes of the compounds were investigated. The compounds 9 (PSE = 4.2), 12 (PSE = 4.1) and 13 (PSE = 3.9) with the highest potency selectivity expression ...[more]

PMID: 28260401

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