Benzocarbazoledinones as SARS-CoV-2 Replication Inhibitors: Synthesis, Cell-Based Studies, Enzyme Inhibition, Molecular Modeling, and Pharmacokinetics Insights.

Endemic and pandemic viruses represent significant public health challenges, leading to substantial morbidity and mortality over time. The COVID-19 pandemic has underscored the urgent need for the development and discovery of new, potent antiviral agents. In this study, we present the synthesis and anti-SARS-CoV-2 activity of a series of benzocarbazoledinones, assessed using cell-based screening assays.

Synthesis and evaluation of hybrid sulfonamide-chalcones with potential antileishmanial activity.

Leishmaniasis is an emerging tropical infectious disease caused by a protozoan parasite of the genus Leishmania. In this work, the molecular hybridization between a trimethoxy chalcone and a sulfonamide group was used to generate a series of sulfonamide-chalcones. A series of eight sulfonamide-chalcone hybrids were made with good yields (up to 95%).

Aurones: A Promising Scaffold to Inhibit SARS-CoV-2 Replication.

Aurones are a small subgroup of flavonoids in which the basic C-C-C skeleton is arranged as ()-2-benzylidenebenzofuran-3(2)-one. These compounds are structural isomers of flavones and flavonols, natural products reported as potent inhibitors of SARS-CoV-2 replication. Herein, we report the design, synthesis, and anti-SARS-CoV-2 activity of a series of 25 aurones bearing different oxygenated groups (OH, OCH, OCHOCH, OCHO, OCFH, and OCHCHR) at the A- and/or B-rings using cell-based screening assays.

Synthesis of new α-Aryl-α-tetralones and α-Fluoro-α-aryl-α-tetralones, preliminary antiproliferative evaluation on drug resistant cell lines and in silico prediction of ADMETox properties.

α-aryl-α-tetralones and α-fluoro-α-aryl-α-tetralones derivatives were synthesized by palladium catalyzed α-arylation reaction of α-tetralones and α-fluoro-α-tetralones, with bromoarenes in moderate to good yields. These compounds were evaluated for their in vitro anti-proliferative effects against human breast cancer and leukemia cell lines with diverse profiles of drug resistance. The most promising compounds, 3b, 3c, 8a and 8c, were effective on both neoplastic models.

Comparison of photobiomodulation in the treatment of skin injury with an open wound in mice.

This study aimed to investigate the effects of photobiomodulation at a wavelength of 660 and 830 nm at different numbers of application points in the healing of open wounds in mice. In total, 120 mice were divided into 10 groups. The animals were submitted to cutaneous lesion of the open wound type (1.

Photobiomodulation promotes neural regeneration when compared to simvastatin treatment in a sciatic nerve crush model.

To determine whether the effects of photobiomodulation (PBM) were associated with the use of Simvastatin in the functional recovery from sciatic nerve in mice submitted to crush injury. Fifty Swiss mice (approximately 3 months old; average weight 40 g) were randomly divided into six groups: naive, sham, control, PBM (660 nm, 10 J/cm; 30 mW; 0.6 J per day for 28 days; 0.

Photobiomodulation in Sciatic Nerve Crush Injuries in Rodents: A Systematic Review of the Literature and Perspectives for Clinical Treatment.

The aim of the study was to perform a literature review to analyze the effect of photobiomodulation in experimental studies on peripheral nerve regeneration after sciatic nerve crush injury in rodents. A bibliographic search was performed in the electronic databases, including MEDLINE (PubMed), SCOPUS, and SciELO, from 2008 to 2018. A total of 1912 articles were identified in the search, and only 19 fulfilled all the inclusion criteria.

Theoretical studies and NMR assay of coumarins and neoflavanones derivatives as potential inhibitors of acetylcholinesterase.

Currently Alzheimer's disease (AD) is a devastating neurological disorder that mainly affects the elderly. The treatment of AD has as main objective to increase the levels of ACh in the synaptic cleft by inhibiting the cholinesterase enzymes, which are responsible for the degradation of ACh. Twenty one synthesized coumarins and neoflavanones (4-arylcoumarins) and theoretical studies were used to select the most promising ligands for in vitro experimental studies by Nuclear Magnetic Resonance.

Comparative effect of photobiomodulation associated with dexamethasone after sciatic nerve injury model.

To analyze the effect of photobiomodulation and dexamethasone on nerve regeneration after a sciatic nerve crushing model. Twenty-six Swiss mice were divided into the following groups: naive; sham; injured, low-level laser therapy (LLLT) (660 nm, 10 J/cm, 0.6 J, 16.

Coumarins as cholinesterase inhibitors: A review.

The first report in literature of the isolation of coumarin was in the year 1820. After this report, other papers were published demonstrating the isolation and synthesis of coumarin and analogues. These compounds have been studying along the years for several different pathologies.