PMID: 17504136May 17, 2007

Malarial parasite carbonic anhydrase and its inhibitors

Current Topics in Medicinal Chemistry
J KrungkraiClaudiu T Supuran

Abstract

Plasmodium falciparum is responsible for the majority of life-threatening cases of human malaria. The global emergence of drug-resistant malarial parasites necessitates identification and characterization of novel drug targets. At present, carbonic anhydrase (CA) genes are identified in limited numbers of protozoa and helminthes parasites, however, they are demonstrated in at least 4 Plasmodium species. The CA gene of P. falciparum encodes an alpha-carbonic anhydrase enzyme possessing catalytic properties distinct of that of the human host enzymes. A small library of aromatic sulfonamides, most of which were Schiff's bases derived from sulfanilamide/homosulfanilamide/4-aminoethylbenzenesulfonamide and substituted-aromatic aldehydes, or ureido-substituted sulfonamides are good inhibitors of P. falciparum enzyme. The 4-(3,4-dichlorophenylureido-ethyl)-benzenesulfonamide is the most effective antimalarial activity against growth of P. falciparum in vitro. The nature of the groups substituting the aromatic-ureido- or aromatic-azomethine fragment of the molecule and the length of the parent sulfonamide (i.e., from sulfanilamide to 4-aminoethylbenzenesulfonamide) from which the Schiff's base obtained, are the critical parameters for ...Continue Reading

Citations

Jun 1, 2011·Asian Pacific Journal of Tropical Biomedicine·S R Krungkrai, J Krungkrai
Aug 3, 2011·Future Medicinal Chemistry·Claudiu T Supuran
Dec 17, 2014·Expert Opinion on Therapeutic Targets·Claudiu T Supuran, Clemente Capasso
Mar 16, 2013·Expert Opinion on Therapeutic Patents·Clemente Capasso, Claudiu T Supuran
Jun 5, 2016·Asian Pacific Journal of Tropical Medicine·S R Krungkrai, J Krungkrai
Jun 7, 2012·Parasitology International·Pablo Bilbao-RamosM Eugenia González-Rosende
Dec 29, 2007·ChemMedChem·Katia D'AmbrosioGiuseppina De Simone
Jul 14, 2016·The Biochemical Journal·Claudiu T Supuran

Related Concepts

Metazoa
Antimalarials
Carbonic Anhydrase Inhibitors
Plasmodium falciparum
Sulfonamides

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