Abstract
An original series of 4-substituted pyrrolo[1,2-a]quinoxaline derivatives, new structural analogues of Galipea species quinoline alkaloids, was synthesized from various substituted 2-nitroanilines via multistep heterocyclizations and tested for in vitro antiparasitic activity upon Leishmania amazonensis and Leishmania infantum strains. Structure-activity relationships enlighten the importance of the 4-substituted alkenyl side chain on the pyrrolo[1,2-a]quinoxaline moiety to modulate the antileishmanial activity.
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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Crystallography, X-Ray
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Humans
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Hydrophobic and Hydrophilic Interactions
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Leishmania / drug effects*
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Leukocytes, Mononuclear / drug effects
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Models, Molecular
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Molecular Structure
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Parasitic Sensitivity Tests
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Quinoxalines* / chemical synthesis
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Quinoxalines* / chemistry
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Quinoxalines* / pharmacology
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Antiprotozoal Agents
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Quinoxalines