showing 13 related works from this author
Epidemiology of intensive care unit-acquired sepsis in Italy: Results of the SPIN-UTI network
2018
Background. Sepsis is the major cause of mortality from any infectious disease worldwide. Sepsis may be the result of a healthcare associated infection (HAI): the most frequent adverse events during care delivery especially in Intensive Care Units (ICUs). The main aim of the present study was to describe the epidemiology of ICU-acquired sepsis and related outcomes among patients enrolled in the framework of the Italian Nosocomial Infections Surveillance in ICUs - SPIN-UTI project. Study design. Prospective multicenter study. Methods. The SPIN-UTI network adopted the European protocols for patient-based HAI surveillance. Results. During the five editions of the SPIN-UTI project, from 2008 to…
Aggregation versus Biological Activity in Gold(I) Complexes. An Unexplored Concept
2021
The aggregation process of a series of mono- and dinuclear gold(I) complexes containing a 4-ethynylaniline ligand and a phosphane at the second coordination position (PR3-Au-C≡CC6H4-NH2, complexes 1-5, and (diphos)(Au-C≡CC6H4-NH2)2, complexes 6-8), whose biological activity was previously studied by us, has been carefully analyzed through absorption, emission, and NMR spectroscopy, together with dynamic light scattering and small-angle X-ray scattering. These experiments allow us to retrieve information about how the compounds enter the cells. It was observed that all compounds present aggregation in fresh solutions, before biological treatment, and thus they must be entering the cells as a…
Development of novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation.
2015
Novel dipeptide-like rhodesain inhibitors containing the 3-bromoisoxazoline warhead in a constrained conformation were developed; some of them possess K(i) values in the micromolar range. We studied the structure-activity relationship of these derivatives and we performed docking studies, which allowed us to find out the key interactions established by the inhibitors with the target enzyme. Biological results indicate that the nature of the P2 and P3 substituents and their binding to the S2/S3 pockets is strictly interdependent.
Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antipr…
2014
Novel papain-family cathepsin L-like cysteine protease inhibitors endowed with antitrypanosomal and antimalarial activity were developed, through an optimization study of previously developed inhibitors. In the present work, we studied the structure-activity relationships of these derivatives, with the aim to develop new analogues with a simplified and more synthetically accessible structure and with improved antiparasitic activity. The structure of the model compounds was significantly simplified by modifying or even eliminating the side chain appended at the C3 atom of the benzodiazepine scaffold. In addition, a simple methylene spacer of appropriate length was inserted between the benzod…
Optimization of peptidomimetic boronates bearing a P3 bicyclic scaffold as proteasome inhibitors
2014
Abstract A new series of pseudopeptide boronate proteasome inhibitors (2–3) was developed, through optimization of our previously described analogs of bortezomib, bearing a bicyclic 1,6-naphthyridin-5(6H)-one scaffold as P3 fragment (1). The biological evaluation on human 20S proteasome displayed a promising inhibition profile, especially for compounds bearing a P2 ethylene fragment, which exhibited Ki values in the nanomolar range for the ChT-L activity (e.g. 2a, Ki = 0.057 μM) and considerable selectivity for proteasome over bovine pancreatic α-chymotrypsin. Docking experiments into the yeast 20S proteasome revealed that the ligands are accommodated predominantly into the ChT-L site and t…
Development of rhodesain inhibitors with a 3-bromoisoxazoline warhead
2013
Novel rhodesain inhibitors were obtained by combining an enantiomerically pure 3-bromoisoxazoline warhead with a specific peptidomimetic recognition moiety. All derivatives behaved as inhibitors of rhodesain, with low micromolar Ki values. Their activity against the enzyme was found to be paralleled by an in vitro antitrypanosomal activity, with IC50 values in the mid-micromolar range. Notably, a preference for parasitic over human proteases, specifically cathepsins B and L, was observed.
Development of Novel Selective Peptidomimetics Containing a Boronic Acid Moiety, Targeting the 20S Proteasome as Anticancer Agents
2014
This paper describes the design, synthesis, and biological evaluation of peptidomimetic boronates as inhibitors of the 20S proteasome, a validated target in the treatment of multiple myeloma. The synthesized compounds showed a good inhibitory profile against the ChT-L activity of 20S proteasome. Compounds bearing a β-alanine residue at the P2 position were the most active, that is, 3-ethylphenylamino and 4-methoxyphenylamino (R)-1-{3-[4-(substituted)-2-oxopyridin-1(2H)-yl]propanamido}-3-methylbutylboronic acids (3 c and 3 d, respectively), and these derivatives showed inhibition constants (Ki ) of 17 and 20 nM, respectively. In addition, they co-inhibited post glutamyl peptide hydrolase act…
Nutritional epigenomic and DNA-damage modulation effect of natural stilbenoids
2023
The aim of the present work is the evaluation of biological effects of natural stilbenoids found in Vitis vinifera, with a focus on their activity as epigenetic modulators. In the present study, resveratrol, pterostilbene and for the first time their dimers (±)-trans-δ-viniferin, (±)-trans-pterostilbene dehydrodimer were evaluated in Caco-2 and HepG-2 cell lines as potential epigenetic modulators. Stilbenoids were added in a Caco-2 cell culture as a model of the intestinal epithelial barrier and in the HepG-2 as a model of hepatic environment, to verify their dose-dependent toxicity, ability to interact with DNA, and epigenomic action. Resveratrol, pterostilbene, and (±)-trans-pterostilbene…
CCDC 2070639: Experimental Crystal Structure Determination
2021
Related Article: Andrea Pinto, Catarina Roma-Rodrigues, Jas S. Ward, Rakesh Puttreddy, Kari Rissanen, Pedro V. Baptista, Alexandra R. Fernandes, Joa��o Carlos Limag, Laura Rodri��guez|2021|Inorg.Chem.|60|18753|doi:10.1021/acs.inorgchem.1c02359
CCDC 2070637: Experimental Crystal Structure Determination
2021
Related Article: Andrea Pinto, Catarina Roma-Rodrigues, Jas S. Ward, Rakesh Puttreddy, Kari Rissanen, Pedro V. Baptista, Alexandra R. Fernandes, Joa��o Carlos Limag, Laura Rodri��guez|2021|Inorg.Chem.|60|18753|doi:10.1021/acs.inorgchem.1c02359
CCDC 963005: Experimental Crystal Structure Determination
2013
Related Article: Roberta Ettari, Lucia Tamborini, Ilenia C. Angelo, Silvana Grasso, Tanja Schirmeister, Leonardo Lo Presti, Carlo De Micheli, Andrea Pinto, Paola Conti|2013|ChemMedChem|8|2070|doi:10.1002/cmdc.201300390
CCDC 2070640: Experimental Crystal Structure Determination
2021
Related Article: Andrea Pinto, Catarina Roma-Rodrigues, Jas S. Ward, Rakesh Puttreddy, Kari Rissanen, Pedro V. Baptista, Alexandra R. Fernandes, João Carlos Limag, Laura Rodríguez|2021|Inorg.Chem.|60|18753|doi:10.1021/acs.inorgchem.1c02359
CCDC 2070638: Experimental Crystal Structure Determination
2021
Related Article: Andrea Pinto, Catarina Roma-Rodrigues, Jas S. Ward, Rakesh Puttreddy, Kari Rissanen, Pedro V. Baptista, Alexandra R. Fernandes, João Carlos Limag, Laura Rodríguez|2021|Inorg.Chem.|60|18753|doi:10.1021/acs.inorgchem.1c02359