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A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode α-carbonic anhydrases

Crocetti, Letizia, Maresca, Alfonso, Temperini, Claudia, Hall, Rebecca A., Scozzafava, Andrea, Mühlschlegel, Fritz A., Supuran, Claudiu T. (2009) A thiabendazole sulfonamide shows potent inhibitory activity against mammalian and nematode α-carbonic anhydrases. Bioorganic & Medicinal Chemistry Letters, 19 (5). pp. 1371-1375. ISSN 0960-894X. (doi:10.1016/j.bmcl.2009.01.038) (The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided) (KAR id:91844)

The full text of this publication is not currently available from this repository. You may be able to access a copy if URLs are provided.
Official URL
https://doi.org/10.1016/j.bmcl.2009.01.038

Abstract

A sulfonamide derivative of the antihelmintic drug thiabendazole was prepared and investigated for inhibition of the zinc enzyme carbonic anhydrase CA (EC 4.2.1.1). Mammalian isoforms CA I-XIV and the nematode enzyme of Caenorhabditis elegans CAH-4b were included in this study. Thiabendazole-5-sulfonamide was a very effective inhibitor of CAH-4b and CA IX (K(I)s of 6.4-9.5nm) and also inhibited effectively isozymes CA I, II, IV-VII, and XII, with K(I)s in the range of 17.8-73.2nM. The high resolution X-ray crystal structure of its adduct with isozyme II evidenced the structural elements responsible for this potent inhibitory activity.

Item Type: Article
DOI/Identification number: 10.1016/j.bmcl.2009.01.038
Divisions: Divisions > Division of Natural Sciences > Biosciences
Depositing User: Becky Hall
Date Deposited: 01 Dec 2021 09:33 UTC
Last Modified: 02 Dec 2021 22:41 UTC
Resource URI: https://kar.kent.ac.uk/id/eprint/91844 (The current URI for this page, for reference purposes)
Hall, Rebecca A.: https://orcid.org/0000-0002-4908-8168
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