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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

Indole-3-glyoxyl tyrosine: synthesis and antimalarial activity against Plasmodium falciparum

Full text
Author(s):
Vasconcelos, Stanley N. S. [1] ; Meissner, Kamila A. [2] ; Ferraz, Witor R. [1] ; Trossini, Gustavo H. G. [1] ; Wrenger, Carsten [2] ; Stefani, Helio A. [1]
Total Authors: 6
Affiliation:
[1] Univ Sao Paulo, Dept Farm, Fac Ciencias Farmaceut, Sao Paulo - Brazil
[2] Univ Sao Paulo, Unit Drug Discovery, Dept Parasitol, Inst Ciencias Biomed, Sao Paulo - Brazil
Total Affiliations: 2
Document type: Journal article
Source: Future Medicinal Chemistry; v. 11, n. 6, p. 525-538, MAR 2019.
Web of Science Citations: 2
Abstract

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 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. (AU)

FAPESP's process: 16/24790-9 - Dissecting Plasmodium falciparum EXP1/GST2 for xenobiotic defence in glucose-6-phosphate dehydrogenase deficiency
Grantee:Kamila Anna Meissner
Support type: Scholarships in Brazil - Post-Doctorate
FAPESP's process: 17/25543-8 - Medicinal chemistry strategies (LBDD and SBDD) in the search of tripanomatides sirtuin 2 inhibitors
Grantee:Gustavo Henrique Goulart Trossini
Support type: Regular Research Grants
FAPESP's process: 12/00424-2 - Synthesis of small libraries using potassium Organotrifluoroborates in Suzuki-Miyaura reactions
Grantee:Helio Alexandre Stefani
Support type: Research Projects - Thematic Grants
FAPESP's process: 12/12807-3 - Analysis of the redox status and its effect on the proliferation of Plasmodium falciparum in genetically different erythrocytes
Grantee:Kamila Anna Meissner
Support type: Scholarships in Brazil - Doctorate
FAPESP's process: 15/26722-8 - Drug discovery against human infectious diseases
Grantee:Carsten Wrenger
Support type: Research Projects - Thematic Grants
FAPESP's process: 13/17960-7 - Functionalization of 3-iodo-(L)-Tyrosine via Suzuki-Miyaura reaction using potassium organotrifluoroborate salts
Grantee:Stanley Nunes Siqueira Vasconcelos
Support type: Scholarships in Brazil - Doctorate