Abstract
A novel series of alkyl- or aralkyl-substituted polyamine analogues was synthesized containing a 3-7-3 polyamine backbone. These analogues were evaluated in vitro, and in one case in vivo, for activity as antitrypanosomal agents, and for activity against opportunistic infection caused by Microsporidia. Compound 21 inhibits trypanosomal growth with an IC(50) as low as 31nM, while compound 24 shows promising activity in vitro against trypanosomes, and against Microsporidia in vitro and in vivo.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Antiprotozoal Agents / chemistry*
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Antiprotozoal Agents / pharmacology
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Cell Line
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Encephalitozoon cuniculi / drug effects
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Inhibitory Concentration 50
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Mice
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Mice, Knockout
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Microsporida / drug effects
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Polyamines / chemistry*
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Polyamines / pharmacology*
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Rabbits
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Structure-Activity Relationship
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Trypanocidal Agents / chemistry*
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Trypanocidal Agents / pharmacology
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Trypanosoma brucei brucei / drug effects
Substances
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Antiprotozoal Agents
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Polyamines
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Trypanocidal Agents