Issue 44, 2010
From the journal:

Chemical Communications

Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted-ureido-benzenesulfonamides and correlate to inhibitor potency†

Fabio Pacchiano,a   Mayank Aggarwal,b   Balendu Sankara Avvaru,b   Arthur H. Robbins,b   Andrea Scozzafava,a   Robert McKenna*b  and  Claudiu T. Supuran*a  

* Corresponding authors

a Department of Biochemistry and Molecular Biology, College of Medicine, University of Florida, Box 100245, Gainesville, USA
E-mail: rmckenna@ufl.edu
Fax: +1 352 392-3422
Tel: +1 352 392-5696

b Università degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
E-mail: claudiu.supuran@unifi.it

Abstract

4-Substituted-ureido benzenesulfonamides showing inhibitory activity against carbonic anhydrase (CA, EC 4.2.1.1) II between 3.3–226 nM were crystallized in complex with the enzyme. Hydrophobic interactions between the scaffold of the inhibitors in different hydrophobic pockets of the enzyme were observed, explaining the diverse inhibitory range of these derivatives.

Graphical abstract: Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted-ureido-benzenesulfonamides and correlate to inhibitor potency

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Article information

DOI
https://doi.org/10.1039/C0CC02707C
Article type
Communication
Submitted
21 Jul 2010
Accepted
20 Sep 2010
First published
05 Oct 2010

Chem. Commun., 2010,46, 8371-8373

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Selective hydrophobic pocket binding observed within the carbonic anhydrase II active site accommodate different 4-substituted-ureido-benzenesulfonamides and correlate to inhibitor potency

F. Pacchiano, M. Aggarwal, B. S. Avvaru, A. H. Robbins, A. Scozzafava, R. McKenna and C. T. Supuran, Chem. Commun., 2010, 46, 8371 DOI: 10.1039/C0CC02707C

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