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

Subramanian, Gowtham and Baburajeev, C. P. and Mohan, C. D. and Sinha, Ameya and Chu, Trang T. T. and Anusha, Sebastian and Ximei, Huang and Fuchs, Julian E. and Bender, Andreas and Rangappa, K. S. and Chandramohanadas, Rajesh and Basappa (2016) Synthesis and in vitro evaluation of hydrazinyl phthalazines against malaria parasite, Plasmodium falciparum. Bioorganic & Medicinal Chemistry Letters, 26 (14). 3300 - 3306.

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Official URL: https://doi.org/10.1016/j.bmcl.2016.05.049

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.

Item Type: Article
Uncontrolled Keywords: Hydralazines, Antimalarials, Dihydroorotate dehydrogenase, , Bronsted acidic ionic liquids
Subjects: C Chemical Science > Chemistry
Divisions: Department of > Chemistry
Depositing User: manjula User
Date Deposited: 20 Jun 2019 06:08
Last Modified: 04 Jul 2019 10:19
URI: http://eprints.uni-mysore.ac.in/id/eprint/3467

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