期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 26, 期 14, 页码 3300-3306出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.05.049
关键词
Hydralazines; Antimalarials; Dihydroorotate dehydrogenase; P. falciparum; Bronsted acidic ionic liquids
资金
- University Grants Commission [41-257-2012-SR]
- Vision Group Science and Technology, Department of Science and Technology [SR/FT/LS-142/2012]
- National Research Foundation, Singapore
- DST Indo-Korea [INT/IndoKorea/122/2011-12]
- Institution of Excellence, University of Mysore
- University of Mysore
- Ministry of Education-Singapore
- [SRLS13049]
- [SUTD-ZJU/RES/02/2013]
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. (C) 2016 Published by Elsevier Ltd.
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