A5025207858- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Synthesis and Biological Evaluation
- Enzyme function and inhibition
- Enzyme Production and Characterization
- Pharmacogenetics and Drug Metabolism
- Pneumocystis jirovecii pneumonia detection and treatment
- Fungal Infections and Studies
- Synthesis and biological activity
- Diabetes Treatment and Management
- Antifungal resistance and susceptibility
- Toxin Mechanisms and Immunotoxins
- Drug Transport and Resistance Mechanisms
Universidade Federal do Rio de Janeiro
2016-2022
Arginase catalyzes the hydrolysis of l -arginine into -ornithine and urea, acting as a key enzyme in biosynthesis polyamines. Leishmania growth survival is dependent on polyamine biosynthesis; therefore, inhibition arginase may be promising therapeutic strategy. Here, we evaluated series thirty-six chalcone derivatives potential inhibitors infantum (LiARG). In addition, activity selected against L. parasites was assessed vitro . Seven compounds exhibited LiARG above 50% at 100 μM. Among...
Inhibition of Leishmania arginase leads to a decrease in parasite growth and infectivity thus represents an attractive therapeutic strategy. We evaluated the inhibitory potential selected naturally occurring phenolic substances on infantum (ARGLi) investigated their antileishmanial activity vivo. ARGLi exhibited Vmax 0.28 ± 0.016 mM/min Km 5.1 1.1 mM for L-arginine. The phenylpropanoids rosmarinic acid caffeic (100 µM) showed percentages inhibition 71.48 0.85% 56.98 5.51%, respectively....
With current drug treatments failing due to toxicity, low efficacy and resistance; leishmaniasis is a major global health challenge that desperately needs new validated targets. Inspired by activity of the natural chalcone 2’,6’-dihydroxy-4’-methoxychalcone (DMC), nitro-analogue, 3-nitro-2’,4’,6’- trimethoxychalcone (NAT22, 1c ) was identified as potent broad spectrum antileishmanial lead. Structural modification provided an alkyne containing chemical probe labelled protein within parasite...
SUMMARY Leishmaniasis are diseases caused by parasites of the genus Leishmania and transmitted to humans bite infected insects subfamily Phlebotominae. Current drug therapy shows high toxicity severe adverse effects. Recently, two oligopeptidases (OPBs) were identified in amazonensis , namely oligopeptidase B (OPB) B2 (OPB2). These OPBs could be ideal targets, since both enzymes expressed all parasite lifecycle not human. This work aimed identify possible dual inhibitors OPB OPB2 from L. ....
Sodium-glucose cotransporter 2 inhibitors (SGLT2i) are the latest class of drugs approved to treat type DM (T2DM). Although adverse effects often caused by a metabolite rather than drug itself, only safety assessment disproportionate metabolites is usually performed, which particular concern for chronic use, such as SGLT2i. Bearing this in mind, silico tools efficient strategies reveal risk metabolites, being endorsed many regulatory agencies. Thereby, goal study was apply methods provide...
Leishmaniasis is a neglected disease caused by protozoa of the genus Leishmania spp., which affects about 1.6 million individuals each year and 500,000 present themselves in visceral form. In Brazil there are 30,000 new cases year. addition, country responsible for 90% reported Visceral Leishmaniasis, this more severe form disease. Allied to these facts, current treatment ineffective, contributing establishment resistant strains. Currently, has several side effects permanent damage health...