Search results for "44"
showing 10 items of 1507 documents
Biomedical Applications of Polylactide (PLA) and Its Copolymers.
2018
n/a
A Novel Series of Acylhydrazones as Potential Anti-Candida Agents: Design, Synthesis, Biological Evaluation and In Silico Studies
2019
In the context of an increased incidence of invasive fungal diseases, there is an imperative need of new antifungal drugs with improved activity and safety profiles. A novel series of acylhydrazones bearing a 1,4-phenylene-bisthiazole scaffold was designed based on an analysis of structures known to possess anti-Candida activity obtained from a literature review. Nine final compounds were synthesized and evaluated in vitro for their inhibitory activity against various strains of Candida spp. The anti-Candida activity assay revealed that some of the new compounds are as active as fluconazole against most of the tested strains. A molecular docking study was conducted in order to evaluate the …
Synthesis and Influence of 3-Amino Benzoxaboroles Structure on Their Activity against Candida albicans
2020
Benzoxaboroles emerged recently as molecules of high medicinal potential with Kerydin®
Synthesis, Properties and Antimicrobial Activity of 5-Trifluoromethyl-2-formylphenylboronic Acid
2020
2-Formylphenylboronic acids display many interesting features, not only from synthetic but also from an application as well as structural points of view. 5-Trifluoromethyl-2-formyl phenylboronic acid has been synthesized and characterized in terms of its structure and properties. The presence of an electron-withdrawing substituent results in a considerable rise in the acidity in comparison with its analogues. In some solutions, the title compound isomerizes with formation of the corresponding 3-hydroxybenzoxaborole. Taking into account the probable mechanism of antifungal action of benzoxaboroles, which blocks the cytoplasmic leucyl-tRNA synthetase (LeuRS) of the microorganism, docking stud…
DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents.
2019
Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, …
Effects of Ultrasound-Assisted Extraction and Solvent on the Phenolic Profile, Bacterial Growth, and Anti-Inflammatory/Antioxidant Activities of Medi…
2020
© 2020 by the authors.
The Antioxidant Potential of White Wines Relies on the Chemistry of Sulfur-Containing Compounds: An Optimized DPPH Assay
2019
The DPPH (2,2-Diphenyl-1-picrylhydrazyl) assay is an easy and efficient method commonly used to determine the antioxidant capacity of many food matrices and beverages. In contrast with red wines, white wines are poorer in antioxidant polyphenolics, and the more hydrophilic sulfur-containing compounds in them may contribute significantly to their antioxidant capacity. The modification of the classical DPPH method, with a methanol-buffer and the measure of EC20 (quantity of sample needed to decrease the initial DPPH concentration by 20%) has shown that sulfur-containing compounds such as cysteine (0.037 ±
Succinobucol’s New Coat — Conjugation with Steroids to Alter Its Drug Effect and Bioavailability
2011
Synthesis, detailed structural characterization (X-ray, NMR, MS, IR, elemental analysis), and studies of toxicity, antioxidant activity and bioavailability of unique potent anti-atherosclerotic succinobucol-steroid conjugates are reported. The conjugates consist of, on one side, the therapeutically important drug succinobucol ([4-{2,6-di-tert-butyl-4-[(1-{[3-tert-butyl-4-hydroxy-5-(propan-2-yl)phenyl]sulfanyl}ethyl)sulfanyl]phenoxy}-4-oxo-butanoic acid]) possessing an antioxidant and anti-inflammatory activity, and on the other side, plant stanol/sterols (stigmastanol, β-sitosterol and stigmasterol) possessing an ability to lower the blood cholesterol level. A cholesterol-succinobucol prodr…
Gluten-free flours from cereals, pseudocereals and legumes: Phenolic fingerprints and in vitro antioxidant properties.
2018
The interest in gluten-free (GF) products increases together with the increase in gluten-sensitive people. However, GF foods might have decreased nutritional quality as compared to the gluten containing counterparts. In this work, an investigation of the phenolic and antioxidant profile in 18 GF flours belonging to legumes, cereals and pseudocereals was achieved. Significant differences could be observed across samples. Total phenolic content was highest in violet rice flours, whereas total anthocyanins were highest in violet, nerone, and black rice flours. FRAP and ORAC antioxidant activities were correlated to phenolic contents and found to be higher in violet rice flours. Metabolomics hi…
Natural Compounds as Sustainable Additives for Biopolymers
2020
In the last few decades, the interest towards natural compounds, coming from a natural source and biodegradable, for biopolymers is always increasing because of a public request for the formulation of safe, eco-friendly, and sustainable materials. The main classes of natural compounds for biopolymers are: (i) naturally occurring fillers (nFil), such as nano-/micro- sized layered alumino-silicate: halloysite, bentonite, montmorillonite, hydroxyapatite, calcium carbonate, etc.; (ii) naturally occurring fibers (nFib), such as wood and vegetable fibers; (iii) naturally occurring antioxidant molecules (nAO), such as phenols, polyphenols, vitamins, and carotenoids. However, in this short review, …