Indole-3-glyoxyl tyrosine: synthesis and antimalarial activity against Plasmodium falciparum
| العنوان: | Indole-3-glyoxyl tyrosine: synthesis and antimalarial activity against Plasmodium falciparum |
|---|---|
| المؤلفون: | Gustavo Henrique Goulart Trossini, Hélio A. Stefani, Witor Ribeiro Ferraz, Kamila Anna Meissner, Stanley N. S. Vasconcelos, Carsten Wrenger |
| المصدر: | Repositório Institucional da USP (Biblioteca Digital da Produção Intelectual) Universidade de São Paulo (USP) instacron:USP |
| سنة النشر: | 2019 |
| مصطلحات موضوعية: | Models, Molecular, Indoles, Population, Plasmodium falciparum, 01 natural sciences, Microbiology, 03 medical and health sciences, Antimalarials, Parasitic Sensitivity Tests, parasitic diseases, Drug Discovery, medicine, Humans, Tyrosine, Malaria, Falciparum, education, 030304 developmental biology, Pharmacology, Indole test, 0303 health sciences, education.field_of_study, biology, Hep G2 Cells, biology.organism_classification, medicine.disease, 0104 chemical sciences, Malaria, 010404 medicinal & biomolecular chemistry, Molecular Medicine, Protozoa, Tyrosine synthesis, VIRULÊNCIA |
| الوصف: | 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. |
| URL الوصول: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::218814ec8df38ee77ea95a02fdfa23af |
| حقوق: | OPEN |
| رقم الأكسشن: | edsair.doi.dedup.....218814ec8df38ee77ea95a02fdfa23af |
| قاعدة البيانات: | OpenAIRE |
| الوصف غير متاح. |