Drug Discovery against<i>Babesia</i>and<i>Toxoplasma</i>

Terkawi, Mohamad Alaa; Igarashi, Ikuo

doi:10.1002/9783527633883.ch24

Cited by 2 publications

(1 citation statement)

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“…The limited arsenal of drugs available against these organisms is insufficient due to the rapid emergence of resistance, as is the case for Plasmodium or incomplete activity, as the case for chronic Toxoplasmosis . Thus, there is a continuous need develop new chemotherapies in order to combat these diseases in a unique mode of action [5,6]. …”

Section: Introductionmentioning

confidence: 99%

A minimalistic approach to develop new anti-apicomplexa polyamines analogs

Panozzo-Zénere

Porta

Arrizabalaga

et al. 2018

European Journal of Medicinal Chemistry

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The development of new chemical entities against the major diseases caused by parasites is highly desired. A library of thirty diamines analogs following a minimalist approach and supported by chemoinformatics tools have been prepared and evaluated against apicomplexan parasites. Different member of the series of N,N′−disubstituted aliphatic diamines shown in vitro activities at submicromolar concentrations and high levels of selectivity against Toxoplasma gondii and in chloroquine-sensitive and resistant-strains of Plasmodium falciparum. In order to demonstrate the importance of the secondary amines, ten N,N,N′,N′−tetrasubstituted aliphatic diamines derivatives were synthesized being considerably less active than their disubstituted counterpart. Theoretical studies were performed to establish the electronic factors that govern the activity of the compounds.

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Section: Introductionmentioning

confidence: 99%