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Synthesis and in vitro evaluation of hydrazinyl phthalazines against malaria parasite, Plasmodium falciparum.

Abstract：

: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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Subramanian G,Babu Rajeev CP,Mohan CD,Sinha A,Chu TTT,Anusha S,Ximei H,Fuchs JE,Bender A,Rangappa KS,Chandramohanadas R,Basappa

doi

10.1016/j.bmcl.2016.05.049

subject

Has Abstract

pub_date

2016-07-15 00:00:00

pages

3300-3306

issue

14

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(16)30534-0

journal_volume

26

pub_type

杂志文章

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