Issue 33, 2015
From the journal:

Chemical Communications

X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors†

Jekaterina Ivanova,‡a   Janis Leitans,‡b   Muhammet Tanc,‡cd   Andris Kazaks,b   Raivis Zalubovskis,*a   Claudiu T. Supuran*cd  and  Kaspars Tarsbe  

* Corresponding authors

a Latvian Institute of Organic Synthesis, Aizkraukles 21, LV-1006 Riga, Latvia
E-mail: raivis@osi.lv
Fax: +371-67550338
Tel: +371-67014826

b Biomedical Research and Study Center, Ratsupites 1, LV-1067 Riga, Latvia

c Università degli Studi di Firenze, NEUROFARBA Department, Section of Pharmaceutical Chemistry, Via Ugo Schiff 6, 50019 Sesto Fiorentino, Florence, Italy
E-mail: claudiu.supuran@unifi.it
Fax: +39-055-4573385
Tel: +39-055-4573005

d Università degli Studi di Firenze, Polo Scientifico, Laboratorio di Chimica Bioinorganica, Rm. 188, Via dellaLastruccia 3, 50019 Sesto Fiorentino, Florence, Italy

e University of Latvia, Faculty of Biology, Department of Molecular Biology, Kronvalda bulv. 4, LV-1010 Riga, Latvia

Abstract

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.

Graphical abstract: X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors

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Article information

DOI
https://doi.org/10.1039/C5CC01854D
Article type
Communication
Submitted
04 Mar 2015
Accepted
20 Mar 2015
First published
20 Mar 2015

Chem. Commun., 2015,51, 7108-7111

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X-ray crystallography-promoted drug design of carbonic anhydrase inhibitors

J. Ivanova, J. Leitans, M. Tanc, A. Kazaks, R. Zalubovskis, C. T. Supuran and K. Tars, Chem. Commun., 2015, 51, 7108 DOI: 10.1039/C5CC01854D

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