1. Synthesis and in vitro antileishmanial efficacy of benzyl analogues of nifuroxazide
- Author
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David D. N'Da, Janine Aucamp, Christina Kannigadu, 35159022 - Kannigadu, Christina, 20505698 - Aucamp, Janine, and 20883072 - N'Da, David Dago
- Subjects
Drug ,Nitrofurans ,medicine.drug_class ,Cytotoxicity ,media_common.quotation_subject ,Antibiotics ,Antiprotozoal Agents ,Pharmacology ,03 medical and health sciences ,0302 clinical medicine ,In vitro ,Benzyl Compounds ,Chlorocebus aethiops ,Drug Discovery ,Hydroxybenzoates ,medicine ,Animals ,Promastigote ,Leishmaniasis ,Vero Cells ,Nitrofuran ,media_common ,Leishmania ,biology ,medicine.disease ,biology.organism_classification ,Nifuroxazide ,Multiple drug resistance ,030220 oncology & carcinogenesis ,030217 neurology & neurosurgery ,medicine.drug - Abstract
Leishmaniasis is a vector‐borne parasitic disease that mostly affects populations in tropical and subtropical countries. There is currently no vaccine to protect against and only a handful of drugs are available to treat this disease. Leishmaniasis is curable, but its eradication and elimination are hindered by the emergence of multidrug resistant strains of the causative pathogens, accentuating the need for new and effective antileishmanial drugs. In search for such agents, nifuroxazide, a clinical antibiotic, was evaluated through investigation of its benzyl analogues for in vitro antileishmanial efficacy against promastigotes of various Leishmania (L.) strains. The monobenzylated analogues 1 and 2 were the most potent of all, possessing nanomolar activities up to 10‐fold higher than the parent drug nifuroxazide against all three tested Leishmania strains. Both analogues stand as antipromastigote hits for further lead investigation into their potential to act as new antileishmanial agents.
- Published
- 2020
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