A5020026115- Synthesis and biological activity
- Research on Leishmaniasis Studies
- Synthesis and Characterization of Heterocyclic Compounds
- Synthesis and Biological Evaluation
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthesis and Reactions of Organic Compounds
- Trypanosoma species research and implications
- Multicomponent Synthesis of Heterocycles
- Synthesis of Tetrazole Derivatives
- HIV/AIDS drug development and treatment
- Synthesis and Reactivity of Heterocycles
- Computational Drug Discovery Methods
- Quinazolinone synthesis and applications
- Herpesvirus Infections and Treatments
- Magnetism in coordination complexes
- Synthesis of heterocyclic compounds
- Organophosphorus compounds synthesis
- Cancer therapeutics and mechanisms
- Metal complexes synthesis and properties
- Biochemical and Molecular Research
- Viral Infections and Vectors
- Crystal structures of chemical compounds
- Phenothiazines and Benzothiazines Synthesis and Activities
- Pneumocystis jirovecii pneumonia detection and treatment
Universidade Federal Fluminense
2014-2024
Brazilian National Association of Graduate Programs in Communication
2019
Santen (Japan)
2019
Rio de Janeiro Federal Institute of Education, Science and Technology
2016
Universidade Federal de Itajubá
2014
Hospitais da Universidade de Coimbra
2014
Universidade Federal de Santa Catarina
2013
Fundação Oswaldo Cruz
2004-2009
Universidade Federal Rural do Rio de Janeiro
2004
Military Institute of Engineering
1983
Three series of 4-anilino-1H-pyrazolo[3,4-b]pyridine-5-carboxylic esters were synthesized as part a program to study potential anti-Leishmania drugs. These compounds obtained by condensation reaction 4-chloro-1H-pyrazolo[3,4-b]pyridine with several aniline derivatives. Some them also an alternative pathway involving Mannich-type reaction. The hydrophobic parameter, log P, was determined shake-flask methodology, and using the Hansch−Fujita addictive fragmental constants. tested against...
Ten 1-phenyl-1H-pyrazolo[3,4-b]pyridine derivatives connected by a linker group to benzenesulfonamide moieties with different substituents in the 4-position were synthesized and assayed against Plasmodium falciparum. These ten compounds exhibited activity vitro chloroquine-resistant clone W2 IC50 values ranging from 3.46 9.30 μM. The most active substituent R2 = Cl or CH3 at moiety lowest IC50. Compounds an R1 CO2Et 5-position of 1H-pyrazolo[3,4-b]pyridine ring presented lower than those CN...
Leishmaniasis is a neglected disease responsible for about 56,000 deaths every year. Despite its importance, there are no effective, safe and proper treatments leishmaniasis due to strain resistance and/or drug side-effects. In this work we report the synthesis, molecular modeling, cytotoxicity antileishmanial profile of series 4-(1H-pyrazol-1-yl)benzenesulfonamides. Our experimental data showed an active some compounds against Leishmania infantum amazonensis. The two L. was similar that...
Chemotherapy for leishmaniasis, diseases caused by protozoa of the genus Leishmania, remains inefficient in several treatments. So there is a need to search new drugs. In this work, we have synthesized 1-aryl-1H-pyrazole-4-carboximidamides derivatives and evaluated antileishmanial activities vitro, as well cytotoxic effects. Structure-activity relationship (SAR) studies were carried out with all compounds series. Compound 2 showed an activity profile that can be improved through medicinal...
A series of new 5‐(1‐aryl‐1 H ‐pyrazole‐4‐yl)‐1 ‐tetrazoles 4a‐l were synthesized via [3 + 2] cycloaddition reaction from 1‐aryl‐1 ‐pyrazole‐4‐carbonitriles 3a‐l , sodium azide and ammonium chloride, using dimethylformamide (DMF) as solvent, in good yields: 64–85%. The structures these newly compounds determined the IR, 1 H‐ 13 C‐NMR spectroscopic data elemental analyses.
Chagas disease is a neglected tropical caused by the flagellated protozoan Trypanosoma cruzi. The current drugs used to treat this have limited efficacy and produce severe side effects. Quinolines, nitrogen heterocycle compounds that form complexes with heme, broad spectrum of antiprotozoal activity are promising class new for chemotherapy. In study, we evaluated series 4-arylaminoquinoline-3-carbonitrile derivatives against all forms cruzi in vitro. Compound 1g showed epimastigote when...
Acyclic nucleosides phosphonates (ANPs) belong to a class of antiviral agents, which exhibited activity against several infections.Tenofovir disoproxyl fumarate (TDF) was the first ANP licensed for use as nucleotide reverse transcriptase inhibitors (NRTI) HIV.TDF is an adenosine-5'-monophosphate analogue and pro-drug (R)-9-(2-phosphonomethoxylpropyl) adenine (PMPA), also known tenofovir (TEN).Currently, one most used drugs in antiretroviral therapy due excellent results reducing viral...
Several new 4-(phenylamino)thieno [2,3-f>]pyridines (6a-e) were synthesized and tested against herpes simplex virus type 1 (HSV-1).For the first time one compound (6a) of this heterocyclic system showed 86% inhibitory indicating that these compounds retain antiviral potency in comparison to parent pirazolo-pyridine derivatives. 5
Newly synthesized pyrazole carbohydrazide derivatives with substituents X = Br/Y NO 2 and /Y Cl were independently investigated in the CBA mouse model of cutaneous leishmaniasis. Animals infected Leishmania amazonensis treated two weeks after parasitic infection carbohydrazides for 45 days. Oral treatment both compounds controlled evolution footpad lesions dissemination parasites to draining lymph nodes. Nitric oxide generation was observed supernatants node cells from mice that these...
Tuberculosis (TB) is one of the top ten causes death worldwide, while Chagas disease (CD) parasitic that kills largest number people in Americas. TB leading cause for patients with AIDS; it 1.5 million and 10 new cases every year. The lack newly developed chemotherapeutic agents insufficient access to health care services a diagnosis increase incidence multidrug-resistant (MDRTB) cases. Although CD was identified 1909, chronic stages still adequate treatment.The purpose this work design...
Several new 3-phenyl and 3-alky 1-l//-pyrazolo[3,4-Z>]pyridine derivatives (3a-e) were prepared evaluated against Vaccinia virus on BSC-40 cells.The 3a, 3b 3d showed an inhibitory activity above 90% at 30 μΜ, 40 μΜ 50 concentrations.
Because there is no vaccine in clinical use, control of Leishmaniasis relies almost exclusively on chemotherapy and the conventional treatments exhibit high toxicity for patients emerging drug resistance. Recently, we showed that oral treatment with synthetic pyrazole carbohydrazide compounds induced lower parasite load draining lymph nodes reduced skin lesion size without causing any toxic effects an experimental murine infection model Leishmania amazonensis. In this study, CBA mice were...
In this research, a series of substituted 5‐(5‐amino‐1‐aryl‐1 H ‐pyrazol‐4‐yl)‐1 ‐tetrazoles were synthesized and evaluated for in vitro antileishmanial activity. Among the derivatives, examined compounds 3b 3l exhibited promising activity against promastigotes amastigotes forms Leishmania amazonensis . The cytotoxicity these was on murine cells, giving access to corresponding selectivity index ( SI ).
Twelve new 1H-pyrazolo[3,4-b]pyridine phosphoramidate derivatives were synthesized under mild conditions by nucleophilic aromatic substitution reaction of aminoalkylphosphoramidates over 4-Cl substituted pyrazolo [3,4-b]pyridine in good yields.The compounds characterized IR, 1 H, 13 C and 31 P NMR spectroscopy HRMS.The crystal structure one compound was solved X-ray diffraction showed a network intermolecular interactions involving groups.