The Development of Novel Compounds Against Malaria: Quinolines, Triazolpyridines, Pyrazolopyridines and Pyrazolopyrimidines.

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2019
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Abstract
Based on medicinal chemistry tools, new compounds for malaria treatment were designed. The scaffolds of the drugs used to treat malaria, such as chloroquine, primaquine, amodiaquine, mefloquine and sulfadoxine, were used as inspiration. We demonstrated the importance of quinoline and non-quinoline derivatives in vitro with activity against the W2 chloroquine-resistant (CQR) clone strain and in vivo against -infected mouse model. Among the quinoline derivatives, new hybrids between chloroquine and sulfadoxine were designed, which gave rise to an important prototype that was more active than both chloroquine and sulfadoxine. Hybrids between chloroquine-atorvastatin and primaquine-atorvastatin were also synthesized and shown to be more potent than the parent drugs alone. Additionally, among the quinoline derivatives, new mefloquine derivatives were synthesized. Among the non-quinoline derivatives, we obtained excellent results with the triazolopyrimidine nucleus, which gave us prototype that inspired the synthesis of new heterocycles. The pyrazolopyrimidine derivatives stood out as non-quinoline derivatives that are potent inhibitors of the dihydroorotate dehydrogenase (DHODH) enzyme. We also examined the pyrazolopyridine and pyrazolopyrimidine nuclei.
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c-s-pinheiro2019themolecules Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors C S Pinheiro, Luiz;M Feitosa, Lívia;O Gandi, Marilia;F Silveira, Flávia;Boechat, Nubia;
Journal molecules
Year 2019
DOI
E4095
URL
Keywords
malaria quinoline p. falciparum pfdhodh chloroquine mefloquine primaquine pyrazolopyridine pyrazolopyrimidine triazolopyrimidine

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