Indole-3-glyoxyl tyrosine: synthesis and antimalarial activity againstPlasmodium falciparum
Aim:More than 40 of the world's population, across 105 countries, live in malaria endemic areas. It is estimated that about 500million cases of malaria and half a million deaths occur per year.Results:Herein, we demonstrate the biological activity of indole-3-glyoxyl tyrosine againstPlasmodium 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. Aim: Results: Plasmodium falciparum Conclusion.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2019 |
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| Erschienen: |
2019 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:11 |
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| Enthalten in: |
Future medicinal chemistry - 11(2019), 6, Seite 525- |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Vasconcelos, Stanley NS [VerfasserIn] |
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| Links: |
FID Access [lizenzpflichtig] |
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| Umfang: |
1 Online-Ressource (14 p) |
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| doi: |
10.4155/fmc-2018-0246 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 520 | |a Aim:More than 40 of the world's population, across 105 countries, live in malaria endemic areas. It is estimated that about 500million cases of malaria and half a million deaths occur per year.Results:Herein, we demonstrate the biological activity of indole-3-glyoxyl tyrosine againstPlasmodium 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. Aim: Results: Plasmodium falciparum Conclusion | ||
| 700 | 1 | |a Meissner, Kamila A |e verfasserin |4 aut | |
| 700 | 1 | |a Ferraz, Witor R |e verfasserin |4 aut | |
| 700 | 1 | |a Trossini, Gustavo HG |e verfasserin |4 aut | |
| 700 | 1 | |a Wrenger, Carsten |e verfasserin |4 aut | |
| 700 | 1 | |a Stefani, Hlio A |e verfasserin |4 aut | |
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