Journal article

Synthesis of New Triazolopyrazine Antimalarial Compounds

Daniel JG Johnson, Ian D Jenkins, Cohan Huxley, Mark J Coster, Kah Yean Lum, Jonathan M White, Vicky M Avery, Rohan A Davis

Molecules | MDPI | Published : 2021

Abstract

A radical approach to late-stage functionalization using photoredox and Diversinate™ chemistry on the Open Source Malaria (OSM) triazolopyrazine scaffold (Series 4) resulted in the synthesis of 12 new analogues, which were characterized by NMR, UV, and MS data analysis. The structures of four triazolopyrazines were confirmed by X-ray crystal structure analysis. Several minor and unexpected side products were generated during these studies, including two resulting from a possible disproportionation reaction. All compounds were tested for their ability to inhibit the growth of the malaria parasite Plasmodium falciparum (3D7 and Dd2 strains) and for cytotoxicity against a human embryonic kidney..

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University of Melbourne Researchers

Grants

Awarded by National Health and Medical Research Council


Awarded by Australian Research Council


Funding Acknowledgements

The authors acknowledge the National Health and Medical Research Council (Grant APP1024314 to R.A.D. and M.J.C.) and the Australian Research Council for support toward NMR and MS equipment (Grant LE140100119) and financial support (Grant LP120200339 to R.A.D.). V.M.A. acknowledges Medicines for Malaria Venture for continual financial support.