Evaluating 5-Nitrothiazoles as Trypanocidal Agents
Author(s) -
Ivan P. O’Shea,
Mohammed Shahed,
Benjamín AguileraVenegas,
Shane R. Wilkinson
Publication year - 2015
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.02006-15
Subject(s) - trypanocidal agent , pharmacology , anti infective agents , medicine , virology , biology , trypanosoma brucei , microbiology and biotechnology , antimicrobial , biochemistry , gene
The growth-inhibitory properties of a 5-nitrothiazole series were evaluated against Trypanosoma brucei. A subset of related compounds displayed the greatest potency toward the parasite while exhibiting little cytotoxic effect on mammalian cells, with this antiparasitic activity dependent on expression of a type I nitroreductase by the trypanosome. We conclude that the 5-nitrothiazole class of nitroheterocyclic drugs may represent a new lead in the treatment of human African trypanosomiasis.
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