A5046494707- Aldose Reductase and Taurine
- Nanoparticle-Based Drug Delivery
- Advanced Drug Delivery Systems
- Biochemical and Molecular Research
- Synthesis and biological activity
- Heme Oxygenase-1 and Carbon Monoxide
- Trypanosoma species research and implications
- Research on Leishmaniasis Studies
- Synthesis and Characterization of Heterocyclic Compounds
- RNA Interference and Gene Delivery
- Computational Drug Discovery Methods
- Prenatal Substance Exposure Effects
- Supramolecular Self-Assembly in Materials
- Inhalation and Respiratory Drug Delivery
- Synthesis and Reactions of Organic Compounds
- Polyamine Metabolism and Applications
- Phytochemicals and Antioxidant Activities
- Eicosanoids and Hypertension Pharmacology
- Synthesis and Biological Evaluation
- Colorectal Cancer Treatments and Studies
- Biochemical effects in animals
- Regulation of Appetite and Obesity
- Gout, Hyperuricemia, Uric Acid
- Cannabis and Cannabinoid Research
- Free Radicals and Antioxidants
Magna Graecia University
2024
University of Modena and Reggio Emilia
2014-2023
Excel Life Sciences (India)
2017
Quantitative BioSciences
2017
National University of Singapore
2014
Weatherford College
2010-2014
INTECS (Italy)
2012
Universität Innsbruck
2000-2005
Recordati (Italy)
2004
University of California, San Francisco
2004
Among the strategies that can lead to discovery of new drugs, identification and use privileged structures, molecular fragments are able interact with more than one target, gained particular attention, in an attempt find drugs a shorter time respect other strategies. These have been identified mainly by empirical observations, target only given protein family, or be more, unrelated targets. This review deals structures not covered recent papers on this topic, emphasizes importance...
Protein conformational change is an important consideration in ligand-docking screens, but it difficult to predict. A simple way account for protein flexibility soften the criterion steric fit between ligand and receptor. more comprehensive expensive method would be sample multiple receptor conformations explicitly. Here, these two approaches are compared. "soft" scoring function was created by attenuating repulsive term Lennard-Jones potential, allowing a closer approach protein. The...
In view of the pharmacological interest in phenolic substances, we have determined total amount anthocyanins and polyphenols present berries several cultivars Ribes, Rubus, Vaccinium genera. The vitro antiradical activity crude extracts on chemically-generated superoxide radicals as well inhibitory towards enzyme xanthine oxidase were studied. All examined showed a remarkably high radicals. activities greater than those expected basis quantities samples. Furthermore, certain oxidase. Ribes...
Flavonoids represent a potential source of new antitrypanosomatidic leads. Starting from library natural products, we combined target-based screening on pteridine reductase 1 with phenotypic Trypanosoma brucei for hit identification. Flavonols were identified as hits, and 16 derivatives was synthesized. Twelve compounds showed EC50 values against T. below 10 μM. Four X-ray crystal structures docking studies explained the observed structure–activity relationships. Compound 2...
The active targeting to alveolar macrophages (AM) is an attractive strategy improve the therapeutic efficacy of 'old' drugs currently used in clinical practice for treatment pulmonary tuberculosis. Previous studies highlighted ability respirable solid lipid nanoparticle assemblies (SLNas), loaded with rifampicin (RIF) and functionalized a novel synthesized mannose-based surfactant (MS), both alone blend sodium taurocholate, efficiently target AM via mannose receptor-mediated mechanism. Here,...
Starting from the inhibitory activity of flavonoid Quercetin, a series 4H-1-benzopyran-4-one derivatives was synthesized and tested for inhibition aldose reductase, an enzyme involved in appearance diabetic complications. Some compounds obtained display similar to that Sorbinil but are more selective than Quercetin with respect closely related enzyme, aldehyde also possess antioxidant activity. Remarkably, these higher pKa values carboxylic acids, characteristic which could make...