Synthesis and in vitro evaluation of hydrazinyl phthalazines against malaria parasite, Plasmodium falciparum.
Bioorg Med Chem Lett
; 26(14): 3300-3306, 2016 07 15.
Article
em En
| MEDLINE
| ID: mdl-27261180
In this report, we describe the synthesis of 1-(Phthalazin-4-yl)-hydrazine using bronsted acidic ionic liquids and demonstrate their ability to inhibit asexual stage development of human malaria parasite, Plasmodium falciparum. Through computational studies, we short-listed chemical scaffolds with potential binding affinity to an essential parasite protein, dihydroorotate dehydrogenase (DHODH). Further, these compounds were synthesized in the lab and tested against P. falciparum. Several compounds from our library showed inhibitory activity at low micro-molar concentrations with minimal cytotoxic effects. These results indicate the potential of hydralazine derivatives as reference scaffolds to develop novel antimalarials.
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MEDLINE
Assunto principal:
Ftalazinas
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Plasmodium falciparum
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Antimaláricos
Idioma:
En
Ano de publicação:
2016
Tipo de documento:
Article