Abstract
The synthesis and anti-leishmanial activity of nitroheteroaryl-1,3,4-thiadiazole-based compounds including 1-[5-(5-nitrofuran-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines and 1-[5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl]-4-aroylpiperazines were described. Most of the synthesized compounds exhibited potent anti-leishmanial activity against both promastigote and amastigote forms of Leishmania major at non-cytotoxic concentrations. In general, 5-nitrofuran derivatives were more active than the corresponding 5-nitrothiophene analogues.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Antiprotozoal Agents / chemical synthesis*
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacology*
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Cells, Cultured
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Furans / chemistry
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Leishmania major / drug effects*
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Macrophages / drug effects
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Mice
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Molecular Structure
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Nitrogen Compounds / chemical synthesis*
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Nitrogen Compounds / chemistry
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Nitrogen Compounds / pharmacology
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Piperazine
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Piperazines / chemical synthesis*
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Piperazines / chemistry
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Piperazines / pharmacology*
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Structure-Activity Relationship
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Thiazoles / chemistry*
Substances
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Antiprotozoal Agents
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Furans
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Nitrogen Compounds
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Piperazines
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Thiazoles
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Piperazine
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furan