A5043421735- Crystallization and Solubility Studies
- X-ray Diffraction in Crystallography
- Synthesis and biological activity
- Synthesis and Reactions of Organic Compounds
- Synthesis and Biological Evaluation
- Tuberculosis Research and Epidemiology
- Cancer therapeutics and mechanisms
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Reactivity of Heterocycles
- Crystal structures of chemical compounds
- HIV/AIDS drug development and treatment
- Quinazolinone synthesis and applications
- Fluorine in Organic Chemistry
- Pneumocystis jirovecii pneumonia detection and treatment
- Crystallography and molecular interactions
- Bioactive Compounds and Antitumor Agents
- Covalent Organic Framework Applications
- Click Chemistry and Applications
- Multicomponent Synthesis of Heterocycles
- Biochemical and Molecular Research
- Metal-Organic Frameworks: Synthesis and Applications
- Pancreatic and Hepatic Oncology Research
- Electrochemical sensors and biosensors
- Trypanosoma species research and implications
- Microscopic Colitis
Universidade Federal do Rio de Janeiro
2011-2025
Instituto Nacional do Câncer
2014-2016
Fundação Oswaldo Cruz
2006-2015
Centre National de la Recherche Scientifique
2013
Hospital Braga
2011
Hospital de São João
2011
Hospitais da Universidade de Coimbra
2008
Several nicotinic and isoniazid derivatives, most of them containing nitro groups were synthesized by our group, evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37 Rv using the Alamar Blue susceptibility test expressed as minimum inhibitory concentration (MIC) mg/mL.The compound 11d exhibited best result (1.2 µg/mL) when compared with first line drugs such (INH) rifampicin (RIP).Therefore this class compounds could be a good starting point to develop...
Abstract COF‐300, an imine‐linked, crystalline, and microporous covalent organic framework, modified by coordination of Pd(OAc) 2 to its walls, afforded a hybrid material, @COF‐300, which was used as efficient heterogeneous catalyst for cross‐coupling reactions. This material showed excellent catalytic activity the phosphine‐free Suzuki–Miyaura, Heck, Sonogashira reactions with low palladium loadings (0.1 mol % Pd). X‐ray photoelectron spectroscopy analysis after reaction that Pd II is...
The carboxylic acid residue in the title compound, C6H4BrNO2, is twisted out of plane other atoms, as indicated by (Br)C—C—C—Ocarbonyl torsion angle −20.1 (9)°. In crystal, supramolecular chains mediated O—H⋯N hydrogen bonds are formed with base vector [201] and C—H⋯O interactions reinforce packing.
Abstract Sustainability in chemistry heavily relies on heterogeneous catalysis. Enzymes, the main catalyst for biochemical reactions nature, are an elegant choice to catalyze due their high activity and selectivity, although they usually suffer from lack of robustness. To overcome this drawback, enzyme‐decorated nanoporous catalysts were developed. Three different approaches Candida antarctica lipase B (CAL‐B) immobilization a covalent organic framework (PPF‐2) employed: physical adsorption...
Ten new mefloquine-oxazolidine derivatives, 4-[(1S,8aR)-3-(aryl)hexahydro[1,3]oxazolo[3,4-a]pyridin-1-yl]-2,8-bis(trifluoromethyl)quinoline (1: aryl=substituted phenyl) and 4-[(1S,8aR)-3-(heteroaryl)hexahydro[1,3]oxazolo[3,4-a]pyridin-1-yl]-2,8-bis(trifluoromethyl)quinoline [2: heteroaryl=5-nitrothien-2-yl (2a); 5-nitrofuran-2-yl (2b) 4H-imidazol-2-yl) (2c)], have been synthesized evaluated against Mycobacterium tuberculosis. Compounds 1f (aryl=3-ethoxyphenyl), 1g...
Two series of N’ (E)-heteroaromatic-isonicotinohydrazide derivatives (3a-f and 4a-b) 1-(7-chloroquinolin-4-yl)-2-[(heteroaromatic)methylene]hydrazone (5a-f 6a-b) have been synthesized evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H 37 Rv. Several compounds were noncytotoxic exhibited significant minimum inhibitory concentration (MIC) (3.12, 2.50, 1.25, or 0.60 μg/mL), which can be compared to that the first-line drugs ethambutol (3.12 μg/mL)...
Functionalized 3-trifluoromethyl-2-isoxazolines and 3-trifluoromethylisoxazoles were easily prepared from trifluoromethyl aldoxime 2 under mild conditions by using DIB as oxidant. Theoretical studies of the reactivity trifluoroacetonitrile oxide 4 toward olefins alkynes carried out. The ring-opened with NaBH NiCl to yield corresponding trifluoromethylated γ-amino alcohols.
Leishmaniasis is a neglected tropical disease caused by Leishmania species. Available therapeutic options have several limitations. The drive to develop new, more potent, and selective antileishmanial agents thus major goal. Herein we report the synthesis biological activity evaluation against promastigote amastigote forms of amazonensis nine 4,8-dimethoxynaphthalenyl chalcones. Compound ((E)-1-(4,8-dimethoxynaphthalen-1-yl)-3-(4-nitrophenyl)prop-2-en-1-one), 4f, was most promising with an...
A 52-year-old man with a 1-year history of lower abdominal pain and constipation was referred to our unit for endoscopic resection large lipoma in the ascending colon, which had been detected by computed tomography (CT). Colonoscopy revealed 50-mm, subepithelial, broad-based, polypoid mass colon ([Fig. 1]). Using an electrocautery snare, we transected upper third unroof lesion 2]). Fat observed extruding from cut surface, consistent diagnostic hypothesis 3]). There were no procedure-related...
The <italic>N</italic>-difluoromethyl triazolo-β-aza-ε-amino acid present in the core of peptides led to constrained conformations due CH–F and NH–F interactions.
Abstract Lamivudine, an L-nucleoside, has been considered the cornerstone of antiretroviral therapy programs considering its favorable efficacy, convenient dosing, and safety profile. The low incidence side effects in comparison with D-nucleoside analogs is due to presence sulfur also stereochemistry difference. Considering importance lamivudine especially acquired immune deficiency syndrome treatment, but hepatitis B infection (HBV), two critical diseases nowadays, purpose this article...
Two series of pyrazinamide (PZA) derivatives have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. Some compounds exhibited minimum inhibitory concentration 50–100 μg/mL, greater than the first line antituberculosis drug PZA Alamar Blue assay (>100 μg/mL). The obtained activities can be considered promising results, which characterizes these as good start points to development new antitubercular agents.
The development of novel pharmaceutical tools to efficiently tackle tuberculosis is the order day due rapid resistant strains
The present article describes a series of eighteen N-[(E)-(hydroxy, methoxy and ethoxy substitutedphenyl) methylidene]isonicotinohydrazide derivatives, which were synthesized evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis, the expressed as minimum inhibitory concentration (MIC) μg/ml. Compounds 2a, 2d-f, 2h exhibited significant (0.31-1.25 μg/ml) when compared with first line drugs such isoniazid (INH) rifampicin (RIP) could be good start point to find...
Abstract Amino alcohols constitute a very useful and versatile class of organic compounds, with important applications in synthetic medicinal chemistry. However, most the procedures described literature for obtainment these considerable limitations can be found, such as drastic conditions, long time reactions, poor yields, purification problems. The present article describes methodology that gives amino N-protected based on reduction acid esters under mild employing NaBH4 presence methanol....
In the last three decades, an increasing number of pathogens resistant to common antibiotics have been a serious threat public health worldwide. Pleuromutilin, its derivatives and others natural products are important in fight against pathogen antibiotics, such as respiratory diseases. The aim current review is highlight most pleuromutilin described literature between years 2007 2009. Keywords: Natural products, drugs, pleuromutilin, diseases