Abstract
Aim: More than 40% of the world's population, across 105 countries, live in malaria endemic areas. It is estimated that about 500 million cases of malaria and half a million deaths occur per year. Results: Herein, we demonstrate the biological activity of indole-3-glyoxyl tyrosine against Plasmodium falciparum, which is the causal agent of the most virulent form of malaria in humans. We developed an efficient synthesis of indole-3-glyoxyl tyrosine derivatives, which were then used as key intermediates in the synthesis of functionalized indole-3-glyoxyl biphenyl tyrosines. Conclusion: In biological testing, the compounds exhibited a parasite growth inhibition of over 85%. A cell viability assay showed low cytotoxicity against human cells, with no significant changes in cell viability, making these compounds potential antimalarials.
Supplementary data
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Financial & competing interests disclosure
The authors gratefully acknowledge financial support from the São Paulo Research Foundation (FAPESP, Grant Numbers 2012/00424-2 to HA Stefani, 2015/26722-8 to C Wrenger and 2017/25543-8 to GHG Trossini; and fellowships 2013/17960-7 to SNS Vasconcelos, and 2012/12807-3 and 2016/24790-9 to KA Meissner) and The National Council for Scientific and Technological Development (CNPq) for a fellowship (306119/2014-5 to HA Stefani; 310232/2017-1 to GHG Trossini). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.
No writing assistance was utilized in the production of this manuscript.