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BioMed Research International
Volume 2014, Article ID 162928, 10 pages
http://dx.doi.org/10.1155/2014/162928
Research Article

Sulfa Drugs as Inhibitors of Carbonic Anhydrase: New Targets for the Old Drugs

1Department of Chemistry, Forman Christian College (A Chartered University), Ferozepur Road, Lahore 54600, Pakistan
2Centre for Advanced Drug Research, COMSATS Institute of Information Technology, Abbottabad 22060, Pakistan

Received 28 February 2014; Revised 19 June 2014; Accepted 15 July 2014; Published 8 September 2014

Academic Editor: Anna Di Fiore

Copyright © 2014 Mariya al-Rashida et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Sulfa drugs are well-known antibacterial agents containing N-substituted sulfonamide group on para position of aniline ring (NH2RSO2NHR′). In this study 2,4-dichloro-1,3,5-triazine derivatives of sulfa drugs, sulfamerazine (1b), sulfaquinoxaline (2b), sulfadiazine (3b), sulfadimidine (4b), and sulfachloropyrazine (5b) (1a5a) were synthesized and characterized. Their carbonic anhydrase inhibition activity was evaluated against bovine cytosolic carbonic anhydrase isozyme II (bCA II). For the sake of comparison the CA inhibition activity of the parent sulfa drugs (1b5b) was also evaluated. A significant increase in CA inhibition activity of sulfa drugs was observed upon substitution with 2,4-dichloro-1,3,5-triazine moiety. Molecular docking studies were carried out to highlight binding site interactions. ADME properties were calculated to evaluate drug likeness of the compounds.