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
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..View full abstract
Awarded by National Health and Medical Research Council
Awarded by Australian Research Council
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.