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, A. 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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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 P Library Assistant |
| Date Deposited: | 20 Jun 2019 06:08 |
| Last Modified: | 17 Jun 2022 10:38 |
| URI: | http://eprints.uni-mysore.ac.in/id/eprint/3467 |
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