Abstract
The synthesis and in vitro antiparasitic activity of twenty-seven novel diazabicycles based on tropolone ethers is presented. The compounds can be readily prepared by means of a high-yielding hetero Diels-Alder reaction using simple and readily available starting materials. Several of the new diazabicycles have in vitro activities against Trypanosoma cruzi, Leishmania donovani, Trypanosoma brucei rhodesiense, and chloroquine-resistant Plasmodium falciparum that are comparable or superior to those of currently employed protozoocidal agents.
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* / adverse effects
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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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Azabicyclo Compounds* / adverse effects
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Azabicyclo Compounds* / chemical synthesis
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Azabicyclo Compounds* / chemistry
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Azabicyclo Compounds* / pharmacology
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Cell Survival / drug effects
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Eukaryota / drug effects*
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Humans
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KB Cells
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Microbial Sensitivity Tests
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Molecular Structure
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Parasitic Sensitivity Tests
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Structure-Activity Relationship
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Tropolone / analogs & derivatives*
Substances
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Antiprotozoal Agents
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Azabicyclo Compounds
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Tropolone