Indira Dennemont

Université Paris-Saclay

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Laura Nogueira de Faria Cardoso

Institut de Chimie des Substances Naturelles

Gwenaëlle Jézéquel

Institut de Chimie des Substances Naturelles

Sandy Desrat

Institut de Chimie des Substances Naturelles

Fanny Roussi

Institut de Chimie des Substances Naturelles

Cécile Apel

Institut de Chimie des Substances Naturelles

Sébastien Pomel

Université Paris-Saclay

Marc Litaudon

Centre National de la Recherche Scientifique

Florent Olivon

Institut de Chimie des Substances Naturelles

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Université Paris-Saclay

Centre National de la Recherche Scientifique

Institut de Chimie des Substances Naturelles

University of Puerto Rico at Carolina

Université Paris-Sud

Centre National pour la Recherche Scientifique et Technique (CNRST)

Laboratoire COBRA

Fundação Oswaldo Cruz

Universidade Federal do Rio de Janeiro

Helmholtz Institute for Pharmaceutical Research Saarland

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Synthesis and Anti-Leishmanial Properties of Quinolones Derived from Zanthosimuline

Molecules (2022)

Gwenaëlle Jézéquel Laura Nogueira de Faria Cardoso Florent Olivon Indira Dennemont Cécile Apel

Quinoline derivatives and especially quinolones are considered as privileged structures in medicinal chemistry and are often associated with various biological properties. We recently isolated a series of original monoterpenyl quinolones from the bark of Codiaeum peltatum. As this extract was found to have a significant inhibitory activity against a Leishmania species, we decided to study the anti-leishmanial potential of this type of compound. Leishmaniasis is a serious health problem affecting more than 12 million people in the world. Available drugs cause harmful side effects and resistance for some of them. With the aim of finding anti-leishmanial compounds, we developed a synthetic strategy to access natural quinolones and analogues derived from zanthosimuline. We showed the versatility of this natural compound toward cyclization conditions, leading to various polycyclic quinolone-derived structures. The natural and synthetic compounds were evaluated against amastigote forms of Leishmania infantum. The results obtained confirmed the interest of this family of natural compounds but also revealed promising activities for some intermediates deriving from zanthosimuline. Following the same synthetic strategy, we then prepared 14 new analogues. In this work, we identified two promising molecules with good activities against intramacrophage L. infantum amastigotes without any cytotoxicity. We also showed that slight changes in amide functional groups affect drastically their anti-parasitic activity.

Amastigote

Quinolone

Quinoline

Amide

10.3390/molecules27227892

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