X-Ray Crystallography-Promoted Drug Design of Carbonic Anhydrase Inhibitors

Chemical Communications 2015
Jekaterīna Ivanova, Raivis Žalubovskis, Muhammet Tanc, Andris Kazaks, Claudiu T. Supuran, Kaspars Tārs, Janis Leitans

1-N-Alkylated-6-sulfamoyl saccharin derivatives were prepared and assayed as carbonic anhydrase inhibitors (CAIs). During X-ray crystallographic experiments an unexpected hydrolysis of the isothiazole ring was evidenced which allowed us to prepare highly potent enzyme inhibitors with selectivity for some isoforms with medical applications. This journal is

DOI
10.1039/c5cc01854d
Hipersaite
http://pubs.rsc.org/en/Content/ArticleLanding/2015/CC/C5CC01854D#!divAbstract

Ivanova, J., Žalubovskis, R., Tanc, M., Kazaks, A., Supuran, C., Tārs, K., Leitans, J. X-Ray Crystallography-Promoted Drug Design of Carbonic Anhydrase Inhibitors. Chemical Communications, 2015, Vol.51, 7108.-7111.lpp. ISSN 1359-7345. Pieejams: doi:10.1039/c5cc01854d

Publikācijas valoda
English (en)