Search results for "DME"
showing 10 items of 156 documents
Precision-cut liver slices: A tool to model the liver ex vivo
2013
D is ea se Precision-cut liver slices: A tool to model the liver ex vivo Peter Olinga1,2,*, Detlef Schuppan2 1Division of Pharmaceutical Technology and Biopharmacy, Departement of Pharmacy, University of Groningen, The Netherlands; 2Molecular and Translational Medicine, Department of Medicine I, University Medical Center, Johannes Gutenberg University Mainz, Germany *Corresponding author. Address: Division of Pharmaceutical Technology and Biopharmacy, Departement of Pharmacy, University of Groningen, The Netherlands. Tel.: + 31 50 363 8373; fax: +31 50 363 2500. *E-mail address: P.Olinga@rug.nl
Predicting and Tuning Physicochemical Properties in Lead Optimization: Amine Basicities
2007
This review describes simple and useful concepts for predicting and tuning the pK(a) values of basic amine centers, a crucial step in the optimization of physical and ADME properties of many lead structures in drug-discovery research. The article starts with a case study of tricyclic thrombin inhibitors featuring a tertiary amine center with pK(a) values that can be tuned over a wide range, from the usual value of around 10 to below 2 by (remote) neighboring functionalities commonly encountered in medicinal chemistry. Next, the changes in pK(a) of acyclic and cyclic amines upon substitution by fluorine, oxygen, nitrogen, and sulfur functionalities, as well as carbonyl and carboxyl derivativ…
Efficacy and Safety of Subthreshold Micropulse Yellow Laser for Persistent Diabetic Macular Edema After Vitrectomy: A Pilot Study
2022
Aim: To examine the effect of subthreshold micropulse yellow laser (SMYL) on best-corrected visual acuity (BCVA), central macular thickness (CMT), and optical coherence tomography angiography (OCT-A) changes in eyes with persistent diabetic macular edema (DME) after pars plana vitrectomy (PPV) for tractional DME (TDME).Patients and Methods: In a comparative study, 95 eyes of 95 consecutive patients with persistent DME were prospectively enrolled. The SMYL group (54 eyes) was treated with SMYL 6 months after PPV, while the control group (41 eyes) was followed up without treatment. BCVA and CMT by OCT were analyzed at baseline and 3 and 6 months. Additionally, parameters such as the vessel de…
Aided phytostabilization using Miscanthus sinensis×giganteus on heavy metal-contaminated soils
2013
Abstract A field experiment was carried out to evaluate the use of red mud, a by-product of the alumina industry, as a soil amendment on highly contaminated soils in the vicinity of a former Pb–Zn smelter in Copșa Mica (Romania). Changes in the distribution of Zn, Cd and Pb in various soil fractions, mobility of heavy metals in the soil, and their uptake and effects on growth and productivity of Miscanthus sinensis × giganteus were evaluated. Uptake of Zn, Cd and Pb was determined in different tissues of M. sinensis × giganteus cultivated in field plots situated at increasing distance from the pollution source and with different levels of contamination and metal availabilities. Soluble meta…
Presence of phosphorylatedO-ribosyl-adenosine In T-ψ-stem of yeast methlonine initiator tRNA
1989
We report in this paper on isolation and characterization of two unknown nucleosides G* and [A*] located in the T-psi-stem of yeast methionine initiator tRNA, using the combined means of HPLC protocols, real time UV-absorption spectrum, and post-run mass spectrometry by electron impact or fast atom bombardment. The G* nucleoside in position 65 was identified as unmodified guanosine. The structure of the unknown [A*] in position 64 was characterized as an isomeric form of O-ribosyl-adenosine by comparison of its chromatographic, UV-spectral and mass spectrometric properties with those of authentic O-alpha-ribofuranosyl-(1"----2')-adenosine isolated from biosynthetic poly(adenosine diphosphat…
From inequitable to sustainable e-waste processing for reduction of impact on human health and the environment
2021
Recycling of electric and electronic waste products (e-waste) which amounted to more than 50 million metric tonnes per year worldwide is a massive and global operation. Unfortunately, an estimated 70 & ndash;80% of this waste has not been properly managed because the waste went from developed to low-income countries to be dumped into landfills or informally recycled. Such recycling has been carried out either directly on landfill sites or in small, often family-run recycling shops without much regulations or oversights. The process traditionally involved manual dismantling, cleaning with hazardous solvents, burning and melting on open fires, etc., which would generate a variety of toxic sub…
The Use of Rule-Based and QSPR Approaches in ADME Profiling: A Case Study on Caco-2 Permeability.
2013
During the early ADME profiling the development of simple, interpretable and reliable in silico tools is very important. In this study, rule-based and QSPR approaches were investigated using a large Caco-2 permeability database. Three permeability classes were determined: high (H), moderate (M) and low (L). The main physicochemical properties related with permeability were ranked as follows: Polar Surface Area (PSA)>Lipophilicity (logP/logD)>Molecular Weight (MW)>number of Hydrogen Bond donors and acceptors>Ionization State>number of Rotatable Bonds>number of Rings. The best rule, based on the combination of PSA-MW-logD (3PRule), was able to identify the H, M and L classes with accuracy of …
Unexpected synthesis by a non-classical Pschorr reaction of 3,5-dimethyl-1-phenyl-1,5-dihydro-4H-pyrazolo[4,3-c]quinolin-4-one, with binding affinity…
2014
The reaction of the diazonium salt 12 derived from N-(2-aminophenyl)-N,3-dimethyl-1-phenyl-1H-pyrazole-5-carboxamide with copper sulfate and sodium chloride in the presence of ascorbic acid afforded the unexpected products 3,5-dimethyl-1-phenyl-1,5-dihydro-4H-pyrazolo[4,3-c]¬quinolin-4-one (17) and N-methyl-2-(3-methyl-1-phenyl-1H-pyrazol-5-yl)aniline (19), accompanied by N-(2-chlorophenyl)-N,3-dimethyl-1-phenyl-1H-pyrazole-5-carboxamide (18). Products 17 and 19 are formed via a non-classical Pschorr reaction. The formation of 17 represents an alternative to the literature synthesis of this biologically active compound. The molecular structure of 18 was confirmed by single-crystal X-ray ana…
Exploring Students’ Metacognitive Knowledge: The Case of Integral Calculus
2020
Previous studies of integral calculus have mainly explored students&rsquo
Quantitative Structure-Antioxidant Activity Models of Isoflavonoids: A Theoretical Study
2015
Seventeen isoflavonoids from isoflavone, isoflavanone and isoflavan classes are selected from Dalbergia parviflora. The ChEMBL database is representative from these molecules, most of which result highly drug-like. Binary rules appear risky for the selection of compounds with high antioxidant capacity in complementary xanthine/xanthine oxidase, ORAC, and DPPH model assays. Isoflavonoid structure-activity analysis shows the most important properties (log P, log D, pKa, QED, PSA, NH + OH ≈ HBD, N + O ≈ HBA). Some descriptors (PSA, HBD) are detected as more important than others (size measure Mw, HBA). Linear and nonlinear models of antioxidant potency are obtained. Weak nonlinear relationship…