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Synthesis and in vitro antileishmanial efficacy of benzyl analogues of nifuroxazide
Author(s) -
Kannigadu Christina,
Aucamp Janine,
N'Da David D.
Publication year - 2021
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.21755
Subject(s) - leishmaniasis , leishmania , in vitro , drug , pharmacology , antibiotics , nitrofuran , microbiology and biotechnology , chemistry , medicine , virology , biology , immunology , parasite hosting , biochemistry , genetics , world wide web , computer science
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.