Publications by authors named "Juliana Oliveira de Souza"
Malaria is an infectious illness, affecting vulnerable populations in Third World countries. Inspired by natural products, indole alkaloids have been used as a nucleus to design new antimalarial drugs. So, eighteen oxindole derivatives, analogues were obtained with moderate to excellent yields.
View Article and Find Full Text PDFBackground: Artemisinin-based combination therapy (ACT) is used as the first-line treatment of uncomplicated malaria caused by the Plasmodium falciparum parasite and chloroquine-resistant Plasmodium vivax parasites. Evidence of resistance to ACT has been reported in Cambodia, and without new and effective anti-malarial agents, malaria burden and mortality will rise.
Methods: The used MolPrint 2D fingerprints and the Tanimoto similarity index were used to perform a structural similarity search within the Malaria Box collection to select diverse molecular scaffolds that are different from artesunate.
Article Synopsis
- Researchers developed a surrogate system for the glycine receptor, a type of human ligand-gated ion channel, to overcome challenges associated with studying membrane-bound proteins and the need for complex multi-subunit structures.
- They substituted specific residues from a stable protein, acetylcholine-binding protein, to create a glycine-binding protein that mimics the binding site of the receptor.
- Various biophysical techniques, including X-ray crystallography, were used to characterize this new protein, making it a promising tool for early-stage drug discovery targeting the heteromeric α/β glycine receptor.
Phthalimide Derivatives with Bioactivity against : Synthesis, Evaluation, and Computational Studies Involving Cytochrome Inhibition.
ACS Omega
August 2018
We describe herein the design and synthesis of -phenyl phthalimide derivatives with inhibitory activities against (sensitive and resistant strains) in the low micromolar range and noticeable selectivity indices against human cells. The best inhibitor, 4-amino-2-(4-methoxyphenyl)isoindoline-1,3-dione (), showed a slow-acting mechanism similar to that of atovaquone. Enzymatic assay indicated that inhibited cytochrome complex.
View Article and Find Full Text PDFThe natural product acivicin inhibits the glutaminase activity of cytidine triphosphate (CTP) synthetase and is a potent lead compound for drug discovery in the area of neglected tropical diseases, specifically trypanosomaisis. A 2.1-Å-resolution crystal structure of the acivicin adduct with the glutaminase domain from Trypanosoma brucei CTP synthetase has been deposited in the RCSB Protein Data Bank (PDB) and provides a template for structure-based approaches to design new inhibitors.
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