A5032301440- Adenosine and Purinergic Signaling
- Trypanosoma species research and implications
- Bioactive Compounds and Antitumor Agents
- Pharmacological Effects of Natural Compounds
- Click Chemistry and Applications
- Research on Leishmaniasis Studies
- Organic Chemistry Cycloaddition Reactions
- Synthesis and Biological Evaluation
Fundação Oswaldo Cruz
2019-2022
Twenty new 2-(1H-pyrazol-1-yl)-1,3,4-thiadiazole analogs were synthetized to develop P2X7 receptor (P2X7R) inhibitors. P2X7R inhibition in vitro was evaluated mouse peritoneal macrophages, HEK-293 cells transfected with hP2X7R (dye uptake assay), and THP-1 (IL-1β release assay). The 1-(5-phenyl-1,3,4-thiadiazol-2-yl)-1H-pyrazol-5-amine derivatives 9b, 9c, 9f, 2-(3,5-dimethyl-1H-pyrazol-1-yl)-5-(4-fluorophenyl)-1,3,4-thiadiazole (11c) showed inhibitory effects IC50 values ranging from 16 122...
There are only two drugs for the treatment of Chagas disease, namely, nifurtimox and benznidazole, that can cause several adverse effects. Despite effectiveness these in disease's acute phase, they not recognized as curative chronic establishing need more effective all stages disease. Cruzain is an enzyme plays a vital role life cycle etiologic agent, protozoan Trypanosoma cruzi, being relevant therapeutic target planning new drugs. Using molecular docking dynamics simulations, we have...