Exploring new structural features of the 4-[(3-methyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzenesulphonamide scaffold for the inhibition of human carbonic anhydrases

Distinto S.;Meleddu R.;Cottiglia F.;Deplano S.;SOUSA SEQUEIRA, ANA LISA;Melis C.;Fois B.;ANGIUS, RICCARDO;Maccioni E.
2019-01-01

Abstract

A library of 4-[(3-methyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulphonamides (EMAC8002a-m) was designed and synthesised to evaluate the effect of substituents in the positions 3 and 4 of the dihydrothiazole ring on the inhibitory potency and selectivity toward human carbonic anhydrase isoforms I, II, IX, and XII. Most of the new compounds preferentially inhibit the isoforms II and XII. Both electronic and steric features on the aryl substituent in the position 4 of the dihydrothiazole ring concur to determine the overall biological activity of these new derivatives.
2019
2019
Inglese
34
1
1526
1533
8
WOS:000482077500001
2-s2.0-85071130359
31431095
https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1654470
Esperti anonimi
internazionale
scientifica
Antitumour agents; carbonic anhydrase inhibitors; dihydrotiazoles; sulphonamide; Carbonic Anhydrase Inhibitors; Carbonic Anhydrases; Dose-Response Relationship, Drug; Humans; Isoenzymes; Models, Molecular; Molecular Structure; Structure-Activity Relationship
no
Distinto, S.; Meleddu, R.; Ortuso, F.; Cottiglia, F.; Deplano, S.; SOUSA SEQUEIRA, ANA LISA; Melis, C.; Fois, B.; Angeli, A.; Capasso, C.; Angius, Ric ...espandi
1.1 Articolo in rivista
info:eu-repo/semantics/article
1 Contributo su Rivista::1.1 Articolo in rivista
262
14
open
Files in This Item:
File Size Format  
Distinto et al.pdf

open access

Description: Articolo principale
Type: versione pre-print
Size 2.33 MB
Format Adobe PDF
View/Open
2.33 MB Adobe PDF View/Open

Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.

Questionnaire and social

Share on:
Impostazioni cookie