Search results for "Farmaceutica"

Responsabilità per danno da farmaco tra gestione del rischio e ruolo delle informazioni

2022

Il contributo, dopo aver analizzato le conseguenze dell’inclusione della responsabilità per i danni da prodotti farmaceutici all’interno del regime della responsabilità del produttore da prodotto difettoso ovvero del paradigma di responsabilità da attività pericolose, indaga criticamente le più recenti decisioni sulla responsabilità del produttore farmaceutico, soffermandosi sulla valenza assunta dalle informazioni. In un contesto in cui le esigenze di protezione della persona richiedono un rafforzamento della tutela del consumatore, sarebbe opportuno, anche alla luce del principio di precauzione, tenere in conto il profilo della gestione del rischio e individuare nuove prospettive di tutel…

Studies On Rosmarinic Acid And Its Derivatives

2017

In Silico Design of New Dual Inhibitors of SARS-CoV-2 MPRO through Ligand- and Structure-Based Methods

2023

The viral main protease is one of the most attractive targets among all key enzymes involved in the life cycle of SARS-CoV-2. Considering its mechanism of action, both the catalytic and dimerization regions could represent crucial sites for modulating its activity. Dual-binding the SARS-CoV-2 main protease inhibitors could arrest the replication process of the virus by simultaneously preventing dimerization and proteolytic activity. To this aim, in the present work, we identified two series’ of small molecules with a significant affinity for SARS-CoV-2 MPRO, by a hybrid virtual screening protocol, combining ligand- and structure-based approaches with multivariate statistical analysis. The B…

Targeting SARS-CoV-2 Main Protease for Treatment of COVID-19: Covalent Inhibitors Structure-Activity Relationship Insights and Evolution Perspectives

2022

The viral main protease is one of the most attractive targets among all key enzymes involved in the SARS-CoV-2 life cycle. Covalent inhibition of the cysteine145 of SARS-CoV-2 MPRO with selective antiviral drugs will arrest the replication process of the virus without affecting human catalytic pathways. In this Perspective, we analyzed the in silico, in vitro, and in vivo data of the most representative examples of covalent SARS-CoV-2 MPRO inhibitors reported in the literature to date. In particular, the studied molecules were classified into eight different categories according to their reactive electrophilic warheads, highlighting the differences between their reversible/irreversible mech…

4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle: A promising scaffold towards bioactive molecules

2020

Abstract The quinazolinone nucleus represents, among the class of fused heterocycles, a very important scaffold to obtain molecules with biological activities. A review of literature revealed how such kind of fused heterocycles, coming from natural or synthetic source, are associated with a wide range of biological activities. This review is mainly directed towards the 4-(3H)-quinazolinones N-3 substituted with a five membered heterocycle in which all the possible combinations of nitrogen, sulfur and oxygen atoms are present.

Selective G-quadruplex stabilizers: Schiff-base metal complexes with anticancer activity

2014

The affinity of three square-planar nickel(II) (1), copper(II) (2) and zinc(II) (3) Schiff-base complexes for wild-type human telomeric (h-Telo) and protooncogene c-myc G-quadruplex (G4) DNA was investigated by UV-visible absorption spectroscopy and circular dichroism. DNA-binding constants (Kb) were determined by spectrophotometric titrations for both G4-DNA and B-DNA. The results obtained point out that the three metal complexes selectively bind G4-DNA with higher affinity, up to two orders of magnitude, with respect to B-DNA. The nickel(II) complex 1 was found to be the most effective G4-DNA stabilizer and the Kb values decrease in the order 1 > 2 ≈ 3. Innovative computational investigat…

Scopolamine Derivatives as Potential Pharmaceuticals with Calixarene-CyclodextrineNanosponges as Drug Carriers

2017

Tropane alkaloids are molecules with a strong biological activity, which are mainly produced by the members offamily Solanaceae, but also found inother plant families (Convolvulaceae, Brasicaceae, Erythroxylaceae andEuphorbiaceae).1 More than 20 active pharmaceutical substances containingthetropane moiety have been industrially produced and applied as mydriatics, antiemetics, antispasmodics, anesthetics and bronchodilators.Nearly all of them are based on the Scopolamine structure.2 In recent years, several researchers aimed their work to the use of supramolecular systems for the inclusion of organic species, such as complex systems based on cyclodextrines or calixarenes.3They have attracted…

Essential oils of three species of scutellaria and their influence on Spodoptera littoralis

2013

Chemical composition of volatile and fixed oils from of Salvia argentea L. (Lamiaceae) growing wild in Sicily.

2015

The chemical compositions of the essential oil and of the non-polar extracts (petroleum ether, dichloromethane) of the aerial parts (flowers, leaves and stems) of Salvia argentea L. were determined by GC-FID and gas chromatography–mass spectrometry analysis. 14-Hydroxy-α-humulene (40.1%) was recognised as the main constituents of the essential oil of S. argentea, together with 1,3,8-p-menthatriene (12.1%), globulol (7.4%) and β-sesquiphellandrene (5.8%). Tritriacontane (9.9% and 14.1%), heptacosane (8.4% and 10.5%), hentriacontane (8.3% and 10.9%), tetradecanal (8.4% and 10.2%) and methyldotriacontane (7.9% and 7.6%) were recognised as the main constituents of the extracts in petroleum …

Chemodiversity of the essential oil from leaves of Abies nebrodensis (Lojac.) Mattei

2016

As activities of the project "Preservation of Abies nebrodensis and restore of Geraci Siculo peatlands", the chemical composition of essential oils, obtained from leaves of Madonie fir, was compared with the ones of essential oils derived from Eurasian species studied up to now