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Treatment and prevention of malaria
Published in David A Warrell, Herbert M Gilles, Essential Malariology, 2017
David A Warrell, William M Watkins, Peter A Winstanley
Pyrimethamine is available only as formulations with either a sulphonamide (sulfadoxine, sulfalene) or, for chemoprophylaxis, with dapsone (Maloprim®, Glaxo-Wellcome). PSD treatment for malaria is a single dose (three tablets for an adult; equivalent to 1.25 mg/kg pyrimethamine and 25 mg/kg sulfadoxine). Many manufacturers now produce tablets containing pyrimethamine 25 mg plus sulfadoxine 500 mg. Pyrimethamine-sulfalene has equivalent efficacy, and tablets are available. A solution containing pyrimethamine 10 mg/mL plus sulfadoxine 200 mg/mL is available for intramuscular injection (Hoffman LaRoche).
Sulfonamides
Published in M. Lindsay Grayson, Sara E. Cosgrove, Suzanne M. Crowe, M. Lindsay Grayson, William Hope, James S. McCarthy, John Mills, Johan W. Mouton, David L. Paterson, Kucers’ The Use of Antibiotics, 2017
Natasha E. Holmes, M. Lindsay Grayson
Sulfonamides and other related drugs (dapsone, sulfamoxole, sulfamethoxazole, sulfadoxine, sulfadiazine) inhibit Plasmodium falciparum and P. vivax in vitro, and infected erythrocytes have been shown to take up more sulfamethoxazole than uninfected erythrocytes, suggesting that the intraparasitic concentrations of these drugs could be much higher than the extracellular concentrations (Zhang and Meshnick, 1991). Sulfamethoxypyrazine has also been incorporated into fixed-dose artesunate combination therapies (ACTs) with pyrimethamine for treatment of malaria (Ayede et al., 2010; Jansen, 2011; Sagara et al., 2009), and sulfalene has been used with amodiaquine and pyrimethamine (Okafor et al., 2010). However, malarial parasites have become sulfonamide resistant in many regions (see section 7, Clinical uses of the drug).
Fluorinated scaffolds for antimalarial drug discovery
Published in Expert Opinion on Drug Discovery, 2020
Charu Upadhyay, Monika Chaudhary, Ronaldo N. De Oliveira, Aniko Borbas, Prakasha Kempaiah, Poonam S, Brijesh Rathi
A new set of 1 H-1,2,4-triazol-3-yl benzenesulfonamide derivatives, 26–40 (Figure 4) was synthesized by Boechat et al. aiming to build a new library of potent antimalarial agents [63]. Computational studies were performed to gain an insight into the molecular properties of these analogues. The docking score between the active site of PfDHPS [64] (Dihydropteroate synthase, a bifunctional enzyme including a sulfonamide in its active site) and the new compounds showed stronger interactions for compounds 26–29 possessing a trifluoromethyl group at the triazole ring except 30 over the unsubstituted triazole analogues, 36–40. Additionally, compounds containing trifluoromethyl group 26–29 had improved docking scores (−88.89 to −93.42 kcal/mol) than sulfalene (−78.78 kcal/mol) and sulfadoxine (−78.01 kcal/mol). As expected, the unsubstituted triazole analogues 36–40 showed weaker intermolecular interaction (−71.79 to −83.85 kcal/mol) compared to the -CF3 substituted triazole analogues. With the exception, halogen-containing compounds, 31–33 (−85 to −89 kcal/mol) and 36–38 (approximately −83.8 kcal/mol), except 37 (−76.15 kcal/mol), had improved docking scores compared to sulfadoxine and sulfalene. In conclusion, the docking studies showed that the fluorinated triazole benzenesulfonamides are promising moieties for the development of new antimalarial drugs [63].
New peptide derived antimalaria and antimicrobial agents bearing sulphonamide moiety
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2019
D. I. Ugwuja, U. C. Okoro, S. S. Soman, R. Soni, S. N. Okafor, D. I. Ugwu
Sulfonamides are widely used in medicinal chemistry because of their low cost, low toxicity and excellent biological activity. For example, sulfadoxine, sulfadiazine and sulfalene are effective malaria drugs that possess sulfonamide groups attached to a heterocyclic ring.