Search results for "Farmaceutica"

showing 10 items of 582 documents

Effects of gamma-irradiation on the alpha-tocopherol and fatty acids content of raw unpeeled almond kernels (Prunus dulcis)

2014

Abstract The present study evaluated fatty acid composition and α-tocopherol content of almond as a function of irradiation dose in order to determine dose levels causing minimal undesirable changes to almonds. Raw unpeeled almonds variety Tuono ( Prunus dulcis (Mill.) D. A. Webb) were irradiated using 60 Co source at dose of 0.5, 1.5, 3, 6, 8 and 10 kGy. Both control and irradiated samples were kept frozen and immediately analyzed. The data obtained showed no change in fatty acid compositions up to a dose of 10 kGy; on the contrary, a general trend observed is that increasing the dose of irradiation resulted in the decrease of α-tocopherol content. The study has shown that irradiation is a…

chemistry.chemical_classificationVitaminSettore CHIM/10 - Chimica Degli AlimentiVitamin Emedicine.medical_treatmentfood and beveragesFatty acidγ irradiationSettore CHIM/08 - Chimica FarmaceuticaPrunus dulcischemistry.chemical_compoundchemistryBiochemistrymedicineAlmonds Gamma irradiation Fatty acids a-TocopherolIrradiationTocopherolFood sciencealpha-TocopherolFood Science
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Novel Sortase A Inhibitors to Counteract Gram-Positive Bacterial Biofilms

2019

Sortase A (SrtA) is a membrane enzyme responsible for the covalent anchoring of surface proteins on the cell wall of Gram-positive bacteria. Nowadays it is considered an interesting target for the development of new anti-infective drugs which aim to interfere with important Gram-positive virulence mechanisms. Along the years, we studied the anti-staphylococcal and anti-biofilm activity of some natural and synthetic polyhalogenated pyrrolic compounds, called pyrrolomycins. Some of them were active on Gram-positive pathogens at a μg/mL range of concentration (1.5-0.045 μg/mL) and showed a biofilm inhibition in the range of 50-80%. [1-3] In light of these encouraging results, herein we present…

chemistry.chemical_classificationbiologyGram-positive virulence mechanismsChemistrySortase ABiofilmlcsh:ASettore BIO/19 - Microbiologia Generalebiology.organism_classificationSettore CHIM/08 - Chimica FarmaceuticaCell wallAnti-infective drugsMembraneEnzymen/aSettore CHIM/03 - Chimica Generale E InorganicaCovalent bondSortase Amental disordersBiophysicslcsh:General WorksAnti-biofilm activityPyrrolomycinsBacteriaGramProceedings
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New more polar symmetrical choline kinase inhibitors II: Study of setting up a new scaffold for the cancer therapy

2015

choline kinase inhibitors cancer therapyCHOLINE KINASE INHIBITORS ANTITUMORALSettore CHIM/08 - Chimica Farmaceutica
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4,5,6,9-tetraidropirrolo[2',3':3,4] cicloepta[1,2-d] isossazoli, procedimento per la loro produzione e loro uso come antitumorali

2016

La presente invenzione riguarda derivati a struttura 4,5,6,9- tetraidropirrolo[2',3':3,4]cicloepta[1,2-d]isossazolica, procedimenti per la loro produzione e il loro uso per la cura di patologie a carattere iperproliferativo comprese quelle di natura neoplastica. I nuovi derivati saggiati al National Cancer Institute di Bethesda su un pannello di circa 60 linee cellulari umane divise in 9 sottopannelli (mammella, ovaie, polmone, colon, SNC, melanoma, leucemia, rene, prostata), hanno mostrato attività antiproliferativa da micro a nanomolare, rivelando alcuni derivati particolarmente promettenti

cicloeptaisossazoli agenti antitumoraliSettore CHIM/08 - Chimica Farmaceutica
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Theoretical Determination Of The pKas Of Betalamic Acid Related To The Free-Radical Scavenger Capacity: Comparison Between Semi-Empirical And Ab Init…

2013

computational methodsfree-radical scavengerpKabetalamic acidSettore CHIM/08 - Chimica Farmaceutica
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Effetto della flessibilità conformazionale sull'equilibrio di interconversione tra aldosi e chetosi

2008

Le reazioni di interconversione tra gli aldosi e i chetosi sono importanti trasformazioni, di interesse biochimico, che si presentano in parecchi stadi sia del catabolismo (glicolisi, via dei pentosofosfati) che dell'anabolismo (ciclo di Calvin) dei glucidi. Il meccanismo di reazione accettato, che coinvolge intermedi 1,2-endiolici, è talvolta riferito come una doppia tautomeria acido-catalizzata. Poiché, d'altro canto, reagenti, prodotti ed intermedi presentano tutti un'elevata flessibilità molecolare, ogni indagine computazionale sufficientemente accurata deve comprendere necessariamente l'analisi conformazionale di ciascun substrato coinvolto nell'equilibrio chimico. Tale analisi è stata…

conformational analysis biochemistrySettore CHIM/08 - Chimica Farmaceutica
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4-cyanopirazoles derivatives as a new class of compounds with potent antifungal activity

2015

Introduction We have reported that some 4-nitrosopyrazoles derivatives displayed in vitro and in vivo potent antifungal activity at no cytotoxic concentration and some of these compounds were 4 times more potent than Amphotericine B and Fluconazole respectively against Cryptococcus Neoformans and C. Krusei. We reported also that the absence of NO group or its replacement with NO2 or NH2 groups gave compounds devoid of antimycotical activity. Aim of the work To better understand the mechanism of action and with the aim of identifying the chemical features responsible for the action, we synthesized and tested a new class of compounds in which the 4-NO group was replaced with 4-CN group having…

cyanopirazoles antifungalSettore CHIM/08 - Chimica Farmaceutica
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Stereoselective Synthesis and Pharmacological Evaluation of 2,4-Bridged Piperidine Derivatives Designed to Activate the κ-Opioid Receptor

2021

endo-configurationdiastereoselective reductive aminationenantiomeric excessstructure-affinity relationshipNOESY spectrumKOR agonistconformational restrictionchiral HPLCSettore CHIM/08 - Chimica Farmaceutica2-azabicyclo[3.3.1]octanecis/trans configuration
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Chemical characterization of Anthemis parlatoreana fresh and dried aerial parts by GC and LC chromatographic techniques and evaluation of the antioxi…

2022

Anthemis parlatoreana was collected in the north west coast of Sicily. Fresh and dried aerial parts were subjected to distillation procedure for the extraction and isolation of essential oils. In both fresh and dried samples, the most abundant chemical classes were ketones and esters, represented to a greater extent by β-thujone and β-artemisia acetate, respectively. In dried vegetable material, a high content of α-pinene and δ3-carene was also registered. Aqueous, methanol and ethyl acetate extracts of aerial parts were also investigated in terms of polyphenolic content and antioxidant potential. All the extracts tested showed a quite different quali-quantitative profile and in terms of ch…

essential oil distillationGC-MS/FIDAnthemis parlatoreanaSettore BIO/02 - Botanica SistematicaHPLC-PDA/MSPlant ScienceSettore BIO/15 - Biologia FarmaceuticaEcology Evolution Behavior and Systematicspolyphenolsterpenes
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Synthesis and Antiproliferative Activity of 2,5-bis(3′-Indolyl)pyrroles, Analogues of the Marine Alkaloid Nortopsentin

2013

2,5-bis(3′-Indolyl)pyrroles, analogues of the marine alkaloid nortopsentin, were conveniently prepared through a three step procedure in good overall yields. Derivatives 1a and 1b exhibited concentration-dependent antitumor activity towards a panel of 42 human tumor cell lines with mean IC50 values of 1.54 μM and 0.67 μM, respectively. Investigating human tumor xenografts in an ex-vivo clonogenic assay revealed selective antitumor activity, whereas sensitive tumor models were scattered among various tumor histotypes.

ex-vivo xenograftsIndolesStereochemistryPharmaceutical ScienceMice NudeAntineoplastic AgentsArticleInhibitory Concentration 50MiceCell Line TumorNeoplasmsDrug Discoverybis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; <i>ex-vivo </i>xenograftsIc50 valuesAnimalsHumansnortopsentin analoguePyrrolesClonogenic assayPharmacology Toxicology and Pharmaceutics (miscellaneous)lcsh:QH301-705.5Tumor Stem Cell AssayMice nudeantitumorAntitumor activityDose-Response Relationship DrugChemistryAlkaloidbis-indolyl-pyrroles; nortopsentin analogues; marine alkaloids; antitumor; ex-vivo xenograftsImidazolesTumor Stem Cell AssaySettore CHIM/08 - Chimica FarmaceuticaXenograft Model Antitumor Assaysbis-indolyl-pyrrolemarine alkaloidHuman tumornortopsentin analogueslcsh:Biology (General)Cell culturebis-indolyl-pyrrolesmarine alkaloidsMarine Drugs
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