Abstract
The development of leishmanicidal quinolines and their in vitro (promastigote and amastigote) and, where applicable, in vivo activities are reviewed. This survey provides a direct comparison of bioactivity across different species(e.g. L. donovani, L. amazonensis, L. chagasi, L infantum), and in different animal models (e.g. L. donovani Balb/c mice and L. donovani infected hamsters). The progress of selected quinolines through pre-clinical development and phase I/II trials, and the lead quinoline drugs sitamaquinine and Imiquimod, are discussed in conjunction with delivery systems and combination therapies.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Aminoquinolines / chemistry
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Aminoquinolines / pharmacology
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Aminoquinolines / therapeutic use
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Animals
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Antiprotozoal Agents / chemistry
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Antiprotozoal Agents / pharmacology
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Antiprotozoal Agents / therapeutic use*
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Clinical Trials as Topic
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Drug Evaluation, Preclinical
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Humans
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Imiquimod
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Leishmania / drug effects
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Leishmaniasis / drug therapy*
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Primaquine / chemistry
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Primaquine / pharmacology
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Primaquine / therapeutic use
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Quinolines / chemistry*
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Quinolines / pharmacology
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Quinolines / therapeutic use
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Structure-Activity Relationship
Substances
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Aminoquinolines
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Antiprotozoal Agents
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Quinolines
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Primaquine
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Imiquimod
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8-aminoquinoline