Synthesis of Potential Antimalarials: Primaquine Analogs

Talati, Swati; Latham, Meagan; Moore, Evan G.; Hargreaves, George W.; Blanton, C. DeWitt

doi:10.1002/jps.2600590411

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Primaquine1

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1970

2022

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Cited by 10 publications

(1 citation statement)

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“…In an initial clinical trial (Ethiopia, 1970), primaquine displayed minor efficacy (1 patient of 7 patients was cured) against diffuse CL [88]. However, an observation that the 2-benzyloxy derivative of primaquine was less toxic [89,90], and toxicity were considered in some of these studies [97,99,101,102]. These delivery systems were aimed at increased effectiveness, prolonged duration of action and / or reduced toxicity of the drug.…”

Section: Primaquinementioning

confidence: 99%

Quinolines as Chemotherapeutic Agents for Leishmaniasis

Reynolds¹,

Loughlin²,

Young

2013

MRMC

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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.

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