A5050369919- HIV/AIDS drug development and treatment
- Synthesis of β-Lactam Compounds
- Synthesis and Catalytic Reactions
- HIV Research and Treatment
- Electrochemical Analysis and Applications
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Synthetic Organic Chemistry Methods
- Pneumocystis jirovecii pneumonia detection and treatment
- Cyclopropane Reaction Mechanisms
- Polymer Surface Interaction Studies
- Fuel Cells and Related Materials
- Chemical synthesis and alkaloids
- Analytical Chemistry and Sensors
- Electrostatics and Colloid Interactions
- Computational Drug Discovery Methods
- Click Chemistry and Applications
- Hepatitis C virus research
- Synthesis and pharmacology of benzodiazepine derivatives
- Biochemical and Molecular Research
- Monoclonal and Polyclonal Antibodies Research
- Asymmetric Synthesis and Catalysis
- Advanced Polymer Synthesis and Characterization
- Cyclization and Aryne Chemistry
- Spectroscopy and Quantum Chemical Studies
University of Coimbra
2017-2024
University of Algarve
2015-2020
Abstract Spirocyclic molecules are widely recognized for their complex three‐dimensional features and structural rigidity. Among this class of molecules, the spiro‐lactams subclass stands out, being extensively explored due to its bioactivity utility in a variety scientific fields such as drug design organic synthesis. Given recognition spirocyclic lactams’ broad potential, several efforts have been engaged on pursuit new synthetic strategies towards these molecules. The present review...
This review gives an insight into the most recent synthetic methodologies towards spiro-γ-lactams, a class of compounds that are present in wide range bioactive and naturally occurring molecules.
Structural modulation of previously identified lead spiro-β-lactams with antimicrobial activity was carried out.The main objective this work to synthesize and evaluate the biological novel spiro-lactams based on compounds activity.The target chiral spiro-γ-lactams were synthesized through 1,3-dipolar cycloaddition reaction a diazo-γ-lactam electron-deficient dipolarophiles. In vitro against HIV Plasmodium wide range evaluated. Among these compounds, one derivative good anti-HIV two promising...
The high burden of malaria and HIV/AIDS prevents economic social progress in developing countries. A continuing need exists for development novel drugs treatment regimens both diseases order to address the tolerability long-term safety concerns associated with current options emergence drug resistance. We describe new spiro-β-lactam derivatives potent (nM) activity against HIV Plasmodium no bacteria yeast. best performing molecule series, BSS-730A, inhibited HIV-1 HIV-2 replication an IC50...
The molecular architecture of spirocyclic compounds has been widely explored within the medicinal chemistry field to obtain new with singular three-dimensional pharmacophoric features and improved bioactivity. Herein, synthesis 68 spirocyclopentene-β-lactams is described, resulting from a rational drug design structural modulation highly promising lead compound BSS-730A, previously identified as having dual antimicrobial activity associated novel mechanism action. Among this diverse library...
In silico methodologies have opened new avenues of research to understanding and predicting drug resistance, a pressing health issue that keeps rising at alarming pace. Sequence-based interpretation systems are routinely applied in clinical context an attempt predict mutation-based resistance thus aid the choice most adequate antibiotic antiviral therapy. An important limitation approaches based on genotypic data exclusively is mutations not considered three-dimensional (3D) structure...
Silica oxides nano- and microparticles, as well silica-based materials, are very abundant in nature industrial processes. Trace metal cation binding with these bulk materials is generally not considered significant speciation studies environmental systems. Nonetheless, this might change for nanoparticulate systems observed a previous study of Pb(II) small SiO 2 particle (7.5 nm diameter). Besides, by those nanoparticles surprisingly characterized heterogeneity that increases the decrease...
A new selective synthetic approach to indole derivatives bearing a tetrazole moiety has been developed. Arynes, generated in situ from o-(trimethylsilyl)aryl triflates and KF, reacted smoothly with 2-(2-benzyl-2H-tetrazol-5-yl)-2H-azirines give 3-(2-benzyl-2H-tetrazol-5-yl)-indole high selectivity. Deprotection of the gave 3-(1H-tetrazol-5-yl)-indole derivatives.
Integrase inhibitors (INIs) are an important class of drugs for treating HIV-2 infection, given the limited number active against this virus. While clinical efficacy raltegravir and dolutegravir is well established, bictegravir infected patients has not been determined. Little information available regarding activity isolates from failing raltegravir-based therapy. In study, we examined phenotypic matched genotypic susceptibility primary raltegravir-naïve raltegravir-failing to raltegravir,...
Over the last 30 years, HIV has grown to a pandemic status with more than 36 million people infected worldwide. Current therapies provide significant improvement in quality of patients' lives, specifically Highly Active Anti-Retroviral Therapy (HAART). Yet, viral resistance development towards anti-HIV medication stands as main obstacle an effective therapy, having also substantial economic impact on healthcare systems Such is primarily related mutations occurring mainly active site key...
One of the main challenges facing development effective anti HIV-1 medicines relates to high mutation rate essential enzymes, such as Protease (HIV1Pr).[1] Pereira Vaz et al. [2] first reported a threonine insertion at position 35 (E35E_T), in HIV1Pr coding region, among treatment-naïve subtype C infected individuals. Undetectable viral loads were attained after antiretroviral therapy individuals, with no associated major mutations, implying null contribution E35E_T resistance....