A5046969441- Research on Leishmaniasis Studies
- Trypanosoma species research and implications
- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Synthesis and biological activity
- Malaria Research and Control
- HIV/AIDS drug development and treatment
- Metal complexes synthesis and properties
- Toxin Mechanisms and Immunotoxins
- Click Chemistry and Applications
- Computational Drug Discovery Methods
- Bioactive Compounds and Antitumor Agents
- HIV Research and Treatment
- Crystallography and molecular interactions
- Synthesis and Catalytic Reactions
- Cancer therapeutics and mechanisms
- Ferrocene Chemistry and Applications
- Traditional and Medicinal Uses of Annonaceae
- Piperaceae Chemical and Biological Studies
- Mosquito-borne diseases and control
- Insect Pest Control Strategies
- Synthesis and Characterization of Heterocyclic Compounds
- Quinazolinone synthesis and applications
- Pneumocystis jirovecii pneumonia detection and treatment
Fundação Oswaldo Cruz
2016-2025
Universidade Federal de Pernambuco
2006-2015
Hospital São Rafael
2014
Centro de Estudos em Psicologia da Saúde
2014
Drexel University
2012-2013
Instituto de Ciências Farmacêuticas
2013
Abstract A substantial challenge worldwide is emergent drug resistance in malaria parasites against approved drugs, such as chloroquine (CQ). To address these unsolved CQ issues, only rare examples of artemisinin (ART)‐based hybrids have been reported. Moreover, protein targets not identified yet, and the reason for superior efficacy still known. Herein, we report synthesis novel ART–isoquinoline ART–quinoline showing highly improved potencies CQ‐resistant multidrug‐resistant P. falciparum...
Malaria is one of the most widespread diseases worldwide. Besides a growing number people potentially threatened by malaria, consistent emergence resistance against established antimalarial pharmaceuticals leads to an urge toward new drugs. Hybridization two chemically diverse compounds into bioactive product successful concept improve properties hybrid drug relative parent and also overcome multidrug resistance. 1,2,3-Triazoles are significant pharmacophore system among nitrogen-containing...
Research in recent years has demonstrated that the Trypanosoma cruzi cysteine protease cruzain (TCC) is a valid chemotherapeutic target, since inhibitors of this affect pathology appropriately. By exploring N-acylhydrazones (NAH) as privileged structures usually present antiparasitic agents, we investigated library 16 NAH bearing 3-(4-substituted-aryl)-1,2,4-oxadiazole scaffold (NAH 3a-h, 4a-h). The vitro bioactivity against epimastigote and trypomastigote forms T. was evaluated, some under...
The nonpolar fraction of an aqueous ethanol extract the roots Arrabidaea brachypoda, a Brazilian medicinal plant, demonstrated significant in vitro activity against Trypanosoma cruzi, parasite responsible for Chagas disease. Targeted isolation active constituents led to three new dimeric flavonoids (1–3), and their structures were elucidated using UV, NMR, HRMS analysis, as well by chemical derivatization. anti-T. cruzi cytotoxicity toward mammalian cells determined these substances....
ABSTRACT Schistosomiasis is a chronic and debilitating disease caused by trematode of the genus Schistosoma affects over 207 million people. Chemotherapy only immediate recourse for minimizing prevalence this involves predominately administration single drug, praziquantel (PZQ). Although PZQ has proven efficacy, there recognized need to develop new drugs as schistosomicides since studies have shown that repeated use drug in areas endemicity may cause temporary reduction susceptibility...
Entry of HIV-1 into host cells remains a compelling yet elusive target for developing agents to prevent infection. A peptide triazole (PT) class entry inhibitor has previously been shown bind gp120, suppress interactions the Env protein at cell receptor binding sites, inhibit infection, and cause envelope spike breakdown, including gp120 shedding and, some variants, virus membrane lysis. We found that gold nanoparticle-conjugated forms triazoles (AuNP-PT) exhibit substantially more potent...
Piplartine (piperlongumine) is a plant-derived molecule that has been receiving intense interest due to its anticancer characteristics target the oxidative stress. In present paper, two novel piplartine-containing ruthenium complexes [Ru(piplartine)(dppf)(bipy)](PF6)2 (1) and [Ru(piplartine)(dppb)(bipy)](PF6)2 (2) were synthesized investigated for their cellular molecular responses on cancer cell lines. We found both are more potent than metal-free piplartine in panel of lines monolayer...
Piplartine (piperlongumine) is a plant-derived compound found in some Piper species that became novel potential antineoplastic agent. In the present study, we synthesized platinum complex containing piplartine derivative cis-[PtCl(PIP-OH)(PPh3)2]PF6 (where, PIP-OH = demethylated derivative; and PPh3 triphenylphosphine) with enhanced cytotoxicity different cancer cells, investigated its apoptotic action human promyelocytic leukemia HL-60 cells. The structure of ligand was characterized by...
We modified the thiazolidinic ring at positions N3, C4, and C5, yielding compounds 6–24. Compounds with a phenyl position 15–19, 22–24, exhibited better inhibitory properties for cruzain against parasite than 2-iminothiazolidin-4-one 5. were able to identify one high-efficacy trypanocidal compound, 2-minothiazolidin-4-one 18, which inhibited activity of proliferation epimastigotes was cidal trypomastigotes but not toxic splenocytes. Having located some structural determinants properties, we...