170,020 research outputs found
Patent evaluation of WO2019209182 (A1) 2019-10-31 (Conjugated Oligoelectrolytes as Antimicrobial Agents)
No full textIntroduction: The insurgence of antibiotic resistance represents one of the biggest public health challenges of our times. During the years, different compounds were developed to fight against resistant bacterial cells, exploiting different mechanisms of action. Areas covered: The patent application describes a set of antimicrobial compounds bearing to the class of the conjugated oligoelectrolytes (COEs). These are molecules characterized by hydrophobic conjugated backbone and terminal polar ionic pendants, able to intercalate into lipid bilayers of bacterial cells. The patent reports the preparation of 15 new compounds and the evaluation of their antimicrobial effect against ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, Enterobacter spp.). Expert opinion: The preparation of the compounds claimed is simple and the preliminary activity data are very interesting. Among the claimed compounds, COE-D8, COE-T42, and COE-T62 have the ability to strongly inhibit the bacterial growth at doses similar to the ones of last resource antibiotics. Unfortunately, no in-vivo data are reported. Moreover, the presence of several quaternary amines limits the potential application of these compounds only to topical uses
ChemInform Abstract: Progress in the Development of Lysine Methyltransferase SETD8 Inhibitors
No full textProgress in the Development of Lysine Methyltransferase SETD8 Inhibitors —
[34 refs. + subrefs.]. — (MILITE, C.; FEOLI, A.; VIVIANO, M.; RESCIGNO, D.;
MAI, A.; CASTELLANO, S.; SBARDELLA*, G.;
ChemMedChem 11 (2016) 16, 1680-1685, http://dx.doi.org/10.1002/cmdc.201600272
; Dip. Farm., Univ. Studi Salerno, I-84084 Fisciano, Salerno, Italy; Eng.) —
Koehle
LA PAZIENTE ASINTOMATICA NELLA PRATICA AMBULATORIALE GINECOLOGICA: VANTAGGI DI UN ADEGUATO APPROFONDIMENTO STRUMENTALE E DI LABORATORIO
No full textGoing Beyond Counting First Authors in Author Co-citation Analysis
No full textThe present study examines one of the fundamental aspects of author co-citation analysis (ACA) - the way co-citation
counts are defined. Co-citation counting provides the data on which all subsequent statistical analyses and mappings
are based, and we compare ACA results based on two different types of co-citation counting - the traditional type that
only counts the first one among a cited work's authors on the one hand and a non-traditional type that takes into
account the first 5 authors of a cited work on the other hand. Results indicate that the picture produced through this non-traditional author co-citation counting contains more coherent author groups and is therefore considerably clearer. However, this picture represents fewer specialties in the research field being studied than that produced through the traditional first-author co-citation counting when the same number of top-ranked authors is selected and analyzed. Reasons for these effects are discussed
Burst-Mode Equalization Strategies in 25 Gbps US-PON using Duobinary and 10G-Class APD for 20-km in C-Band
No full text25 Gbps burst-mode upstream duobinary transmission in C-band using 10G optoelectronics and APD-based adaptive equalization receiver is analyzed and experimentally demonstrated. We show a memory-aided alternative that avoids the long training preambles (>2600 bits) needed in commonly proposed memoryless approaches
Mitomycin C in highly myopic eyes - Author reply
No full textOphthalmology. 2005 Feb;112(2):208-18; discussion 219.
Mitomycin C modulation of corneal wound healing after photorefractive keratectomy in highly myopic eyes.
Gambato C, Ghirlando A, Moretto E, Busato F, Midena E.
SourceRefractive Surgery Service and Antimetabolite Therapy Research Unit, Department of Ophthalmology, University of Padova, Padova, Italy.
Abstract
PURPOSE: To evaluate the role of topical mitomycin C in corneal wound healing (CWH) after photorefractive keratectomy (PRK) in highly myopic eyes.
DESIGN: Prospective, double-masked, randomized clinical trial.
PARTICIPANTS: Seventy-two eyes of 36 patients affected by high (>7 diopters) myopia.
METHODS: In each patient, one eye was randomly assigned to PRK with intraoperative topical 0.02% mitomycin C application, and the fellow eye was treated with a placebo. Postoperatively, mitomycin C-treated eyes received artificial tears (3 times daily, tapered in 3 months), whereas the fellow eye was treated with fluorometholone sodium 2% and artificial tears (3 times daily, tapered in 3 months).
MAIN OUTCOME MEASURES: Uncorrected visual acuity (UCVA) and best-corrected visual acuity (BCVA), contrast sensitivity, manifest refraction, and biomicroscopy. Contrast sensitivity was determined using the Pelli-Robson chart. Corneal confocal microscopy documented CWH.
RESULTS: Mean follow-up was 18 months (range, 12-36). No side effects or toxic effects were documented. At 12-month follow-up examination, UCVAs (logarithm of the minimum angle of resolution) were 0.4+/-0.48 and 0.5+/-0.53 (P = .03) in mitomycin C-treated eyes and corticosteroid-treated eyes, respectively. At 1 year, corneal haze developed in 20% of corticosteroid-treated eyes, versus 0% of mitomycin C-treated eyes. At 12, 24, and 36 months, corneal confocal microscopy showed activated keratocytes and extracellular matrix significantly more evident in untreated eyes (Ps = 0.004, 0.024, and 0.046, respectively).
CONCLUSION: Topical intraoperative application of 0.02% mitomycin C can reduce haze formation in highly myopic eyes undergoing PRK.
Comment in
Ophthalmology. 2006 Feb;113(2):357; author reply 357-8
Dispelling the Myths Behind First-author Citation Counts
No full textWe conducted a full-scale evaluative citation analysis study of scholars in the XML research field to explore just how different from each other author rankings resulting from different citation counting methods actually are, and to demonstrate the capability of emerging data and tools on the Web in supporting more realistic citation counting methods. Our results contest some common arguments for the continued
use of first-author citation counts in the evaluation of scholars, such as high correlations between author rankings by first-author citation counts and other citation
counting methods, and high costs of using more realistic citation counting methods that are not well-supported by the ISI databases. It is argued that increasingly available digital full text research papers make it possible for citation analysis studies to go beyond what the ISI databases have directly supported and to employ more
sophisticated methods
Design, synthesis and in vitro evaluation of bivalent chemical probes for bromo and extra-terminal domain (BET) proteins
No full textBromodomains (BRDs) are epigenetic readers that specifically recognize the acetyl-lysine residues of histones. The role in chromatin remodeling and transcriptional regulation correlate these proteins to several disease states such cancer, inflammation, and viral infection, making them an excellent therapeutic target. The most studied and druggable family of BRD-containing proteins is the bromo and extra C-terminal domain (BET), whose members (BRD2, BRD3, BRD4, and BRDT) contain two highly homologous bromodomains: BD1 and BD2. Several reports have suggested that these domains have different functions and their selective inhibition could be beneficial in treating diseases or mitigating unwanted effects. To date, despite the extensive efforts, there is still a lack of powerful and selective inhibitors of bromodomain proteins, mainly due to the high homology not only between BET proteins but also between BD1 and BD2 domains. Here we describe the design, synthesis and preliminary biochemical evaluation of a new class of bivalent chemical probes of BET proteins. Using different spacers, we linked two different scaffolds: the RVX-208, a selective inhibitor of BD2 domain and a triazolobenzotriazepine-based compound, an inhibitor of BD1 domain. These compounds, simultaneously binding either BD1 or BD2 domains, will help clarify the differences between BD1 and BD2, allowing to get additional details on how these portions recognize the acetylated lysine residues of histones and other proteins
Expanding the quinazoline ring to 3H-benzo[e][1,4]diazepine: development of new and selective G9a inhibitors
No full textHistone lysine methyltransferases have crucial roles in a number of biological processes and human diseases by controlling gene expression and chromatin state. Within this family, the lysine methyltransferase G9a has emerged as a critical player in several pathologic states, mainly due to its important role in the silencing of tumour suppressor genes and in the regulation of other chromatin events (1). Despite the extensive research for new chemical entities, to date there is a low number of G9a chemical probes suitable for cell-based and animal studies, only bearing to the quinazoline class and among all the UNC0638 is the most used and best characterized compound (2).
Keeping this in mind and pursuing our efforts toward the identification of potent and selective histone lysinemethyltransferases inhibitors, we replaced the quinazoline moiety of the UNC0638 with a benzodiazepine framework, obtaining the EML741.
Herein we present the design and synthesis of the EML741 and its inhibitory activity toward G9a HMTase as well as its selectivity profile on other epigenetic enzymes. Moreover, we report the ability of EML741 to lower the G9a activity level in tumor cell lines
Microwave-Assisted Aminoalkylation of Phenols via Mustard Carbonate Analogues
No full textA microwave-assisted chlorine-free direct phenol substitution is presented, which is indicated as a key green chemistry research area for pharmaceuticals manufacturers. The reaction of -aminocarbonates (mustard carbonates) with several substituted phenols in the presence of a polar solvent (acetonitrile or butanol) led to the related aminoalkylated products via the anchimeric assistance of the nitrogen incorporated in the organic carbonate backbone. The aminoalkylation required short reaction time (7 min) and the related products were isolated in high yields (90%) via quick liquid-liquid extraction or column chromatography depending on the solvent employed. Furthermore, microwave irradiation also promoted the one-pot aminoalkylation of phenol in excellent yield. In this approach a -aminoalcohol was reacted with phenol in the presence of diethyl carbonate, used for the in situ formation -aminocarbonate, key intermediate in the consequent anchimerically driven alkylation. The resulting product, namely N,N-dimethyl-2-phenoxyethanamine, was isolated as pure in almost quantitative yield
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