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https://www.readbyqxmd.com/read/27936300/efficient-synthesis-of-trifluoromethyl-amines-through-a-formal-umpolung-strategy-from-the-bench-stable-precursor-me4-n-scf3
#1
Thomas Scattolin, Kristina Deckers, Franziska Schoenebeck
Reported herein is the one-pot synthesis of trifluoromethylated amines at room temperature using the bench-stable (Me4 N)SCF3 reagent and AgF. The method is rapid, operationally simple and highly selective. It proceeds via a formal umpolung reaction of the SCF3 with the amine, giving quantitative formation of thiocarbamoyl fluoride intermediates within minutes that can readily be transformed to N-CF3 . The mildness and high functional group tolerance render the method highly attractive for the late-stage introduction of trifluoromethyl groups on amines, as demonstrated herein for a range of pharmaceutically relevant drug molecules...
December 9, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27936038/abuse-and-diversion-of-immediate-release-opioid-analgesics-as-compared-to-extended-release-formulations-in-the-united-states
#2
Janetta L Iwanicki, S Geoff Severtson, Heather McDaniel, Andrew Rosenblum, Chunki Fong, Theodore J Cicero, Matthew S Ellis, Steven P Kurtz, Mance E Buttram, Richard C Dart
BACKGROUND: Therapeutic use and abuse of prescription opioids in the United States increased substantially between 1990 and 2010. The Centers for Disease Control estimated deaths related to pharmaceutical opioids reached nearly 19,000 in 2014. Of prescription opioids sold, 10% are extended release (ER) and 90% immediate release (IR). However, most regulations and interventions have focused on decreasing ER abuse. Our objective was to compare rates of abuse and diversion of ER and IR opioid analgesics over time using multiple surveillance programs...
2016: PloS One
https://www.readbyqxmd.com/read/27935137/regulation-mechanism-of-pdk1-on-macrophage-metabolism-and-function
#3
REVIEW
Yueqin Yang, Weiwei Kong, Zhi Xia, Lin Xiao, Song Wang
PDK1 is a member of the atypical glandular cell kinases family that regulates the activities of most atypical glandular cell kinases during different development stages and treatment of cancers. PDK1 is also a critical glucose metabolism enzyme regulating glucolysis or glucose oxidase in cells, and more research is needed to further understand the underlying mechanism. The research of PDK1 presented by recent studies focuses much on cancer treatment and has helped researchers gain much insight in this regard...
December 2016: Cell Biochemistry and Function
https://www.readbyqxmd.com/read/27934977/real-time-observation-of-protein-aggregates-in-pharmaceutical-formulations-using-liquid-cell-electron-microscopy
#4
Lynn M DiMemmo, A Cameron Varano, Jonathan Haulenbeek, Yanping Liang, Kaya Patel, Madeline J Dukes, Songyan Zheng, Mario Hubert, Steven P Piccoli, Deborah F Kelly
Understanding the properties of protein-based therapeutics is a common goal of biologists and physicians. Technical barriers in the direct observation of small proteins or therapeutic agents can limit our knowledge of how they function in solution and in the body. Electron microscopy (EM) imaging performed in a liquid environment permits us to peer into the active world of cells and molecules at the nanoscale. Here, we employ liquid cell EM to directly visualize a protein-based therapeutic in its native conformation and aggregate state in a time-resolved manner...
December 9, 2016: Lab on a Chip
https://www.readbyqxmd.com/read/27934635/metabolism-of-the-mek1-2-inhibitor-pimasertib-involves-a-novel-conjugation-with-phospho-ethanolamine-in-patients-with-solid-tumors
#5
Holger Scheible, Friedrich Kraetzer, Andreas Marx, Andreas Johne, Elmar Wimmer
Pimasertib (AS703026 or MSC1936369B) is a selective inhibitor of MEK1/2, the mitogen-activated protein kinase (MAPK) signaling pathway, which is often dysregulated in cancer cells. Pimasertib has shown potent preclinical anti tumor activity and its clinical activity is being investigated in various tumor types. In this phase I study, the disposition and biotransformation of (14)C-radiolabeled pimasertib was investigated in six patients with locally advanced or metastatic solid tumors (NCT 01713036). Ultra-performance liquid chromatography-mass spectrometry (UPLC-MS) and radiodetection techniques were used to investigate the profiles and structures of metabolites in plasma, urine and feces after a single oral dose of (14)C-pimasertib...
December 1, 2016: Drug Metabolism and Disposition: the Biological Fate of Chemicals
https://www.readbyqxmd.com/read/27934549/burden-of-illness-and-research-investments-in-translational-sciences-for-pharmaceuticals-in-metastatic-cancers
#6
Wei-Jhih Wang, Justin C Robertson, Anirban Basu
AIM: To explore whether investments in translational sciences for six metastatic cancers follow idiosyncratic returns to those investments rather than levels of burden of illness (BI). METHODS: Associate the number of translational clinical trials in the USA involving oncolytic drugs approved during 2008-2013 and the level (in 2008) and changes (2002-2008 and 2008-2014) in cancer-specific years of life lost. RESULTS: Investments in trials were positively associated only with contemporary changes in BI (2008-2014)...
December 9, 2016: Journal of Comparative Effectiveness Research
https://www.readbyqxmd.com/read/27934482/pronounced-cellular-uptake-of-pirarubicin-versus-that-of-other-anthracyclines-comparison-of-hpma-copolymer-conjugates-of-pirarubicin-and-doxorubicin
#7
Hideaki Nakamura, Eva Koziolová, Petr Chytil, Kenji Tsukigawa, Jun Fang, Mamoru Haratake, Karel Ulbrich, Tomáš Etrych, Hiroshi Maeda
Many conjugates of water-soluble polymers with biologically active molecules were developed during the last two decades. Although, therapeutic effects of these conjugates are affected by the properties of carriers, the properties of the attached drugs appear more important than the same carrier polymer in this case. Pirarubicin (THP), a tetrahydropyranyl derivative of doxorubicin (DOX), demonstrated more rapid cellular internalization and potent cytotoxicity than DOX. Here, we conjugated the THP or DOX to N-(2-hydroxypropyl)methacrylamide copolymer via a hydrazone bond...
December 5, 2016: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/27934465/recent-developments-in-amide-synthesis-using-nonactivated-starting-materials
#8
Andrea Ojeda-Porras, Diego Gamba-Sánchez
Amides are unquestionably one of the most important functional groups in organic chemistry because of their presence in numerous interesting molecules such as peptides, pharmaceutical agents, naturally occurring molecules, proteins and alkaloids, among others. This synopsis surveys the diverse recent approaches to amide synthesis from nonactivated carboxylic acids and derivatives as well as noncarboxylic compounds, highlighting the most innovative methodologies and those that are more eco-friendly compared to traditional methods while focusing on recent developments during the past two years...
December 2, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27934454/a-reagent-controlled-phospha-michael-addition-reaction-of-nitroalkenes-with-bifunctional-n-heterocyclic-phosphine-nhp-thioureas
#9
Hai Huang, Jake Palmas, Jun Yong Kang
Bifunctional N-heterocyclic phosphine (NHP)-thioureas have been successfully applied for phospha-Michael addition reaction of nitroalkenes to afford diversely substituted β-nitrodiazaphosphonates. This transformation takes place at room temperature under catalyst-free conditions and exhibits broad functional group tolerance. The key to success in catalyst, additive-free reaction conditions is the suitable hydrogen-bond activation of the nitro group by a Brønsted acid (thiourea), which artfully combined with the highly nucleophilic NHP motif for a synergetic effect...
December 2, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27934140/a54-peptide-modified-and-redox-responsive-glucolipid-conjugate-micelles-for-intracellular-delivery-of-doxorubicin-in-hepatocarcinoma-therapy
#10
Na Liu, Yanan Tan, Yingwen Hu, Tingting Meng, Lijuan Wen, Jingwen Liu, Bolin Cheng, Hong Yuan, Xuan Huang, Fuqiang Hu
Redox-responsive nanomaterials applied in drug delivery systems (DDS) have attracted an increasing attention in pharmaceutical research as a carrier for antitumor therapy. However, there would be unwanted drug release from a redox-responsive DDS with no selection at nontarget sites, leading to undesirable toxicities in normal tissues and cells. Here, an A54 peptide modified and PEGylated reduction cleavable glucolipid conjugate (A54-PEG-CSO-ss-SA, abbreviated to APCssA) was designed for intracellular delivery of doxorubicin (DOX)...
December 7, 2016: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/27934015/the-b12-radical-sam-enzyme-poyc-catalyzes-valine-c%C3%AE-methylation-during-polytheonamide-biosynthesis
#11
Aubérie Parent, Alain Guillot, Alhosna Benjdia, Gwladys Chartier, Jérôme Leprince, Olivier Berteau
Genomic and metagenomic investigations have recently led to the delineation of a novel class of natural products called ribosomally synthesized and post-translationally modified peptides (RiPPs). RiPPs are ubiquitous among living organisms and include pharmaceutically relevant compounds such as antibiotics and toxins. A prominent example is polytheonamide A, which exhibits numerous post-translational modifications, some of which were unknown in ribosomal peptides until recently. Among these post-translational modifications, C-methylations have been proposed to be catalyzed by two putative radical S-adenosylmethionine (rSAM) enzymes, PoyB and PoyC...
December 7, 2016: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/27933900/-13-c-nmr-and-lc-ms-profiling-of-stilbenes-from-elicited-grapevine-hairy-root-cultures
#12
Leo-Paul Tisserant, Jane Hubert, Michelle Lequart, Nicolas Borie, Nicolas Maurin, Serge Pilard, Philippe Jeandet, Aziz Aziz, Jean-Hugues Renault, Jean-Marc Nuzillard, Christophe Clément, Michèle Boitel-Conti, Eric Courot
Resveratrol and related oligostilbenes are defense molecules produced by grapevine in response to stresses including various elicitors or signal molecules. Together with their prominent role in planta, these compounds have been the center of much attention in recent decades due to their pharmacological properties. The cost-effective production of resveratrol derivatives such as viniferins or more structurally complex stilbene oligomers remains a challenging task. In this study, the chemical diversity of stilbenes produced by Vitis vinifera Pinot Noir hairy roots was investigated after elicitation for 4 days with a mixture of methyl jasmonate (100 μM) and cyclodextrins (50 mM)...
November 23, 2016: Journal of Natural Products
https://www.readbyqxmd.com/read/27933808/accurate-modeling-of-scaffold-hopping-transformations-in-drug-discovery
#13
Lingle Wang, Yuqing Deng, Yujie Wu, Byungchan Kim, David N LeBard, Dan Wandschneider, Mike Beachy, Richard A Friesner, Robert Abel
The accurate prediction of protein-ligand binding free energies remains a significant challenge of central importance in computational biophysics and structure-based drug design. Multiple recent advances including the development of greatly improved protein and ligand molecular mechanics force fields, more efficient enhanced sampling methods, and low-cost powerful GPU computing clusters have enabled accurate and reliable predictions of relative protein-ligand binding free energies through the free energy perturbation (FEP) methods...
December 9, 2016: Journal of Chemical Theory and Computation
https://www.readbyqxmd.com/read/27933699/room-temperature-arylation-of-thiols-breakthrough-with-aryl-chlorides
#14
Min Jiang, Haifang Li, Haijun Yang, Hua Fu
The formation of aryl C-S bonds is an important chemical transformation because aryl sulfides are valuable building blocks for the synthesis of biologically and pharmaceutically active molecules and organic materials. Aryl sulfides have traditionally been synthesized through the transition-metal-catalyzed cross-coupling of aryl halides with thiols. However, the aryl halides used are usually bromides and iodides; readily available, low-cost aryl chlorides often not reactive enough. Furthermore, the deactivation of transition-metal catalysts by thiols has forced chemists to use high catalyst loadings, specially designed ligands, high temperatures, and/or strong bases, thus leading to high costs and the incompatibility of some functional groups...
December 9, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27933575/-fast-acting-insulin-new-developments-towards-more-flexibility-for-the-patient
#15
Gerhard W Schmeisl, Yasmin Kretzschmar
BACKGROUND: Post-prandial insulin secretion occurs under physiological conditions very fast and in adequate concentrations. This mechanism is impaired in patients with type 2 diabetes and severe increases of postprandial glucose levels may occur. In order to achieve physiological conditions and to avoid postprandial hyperglycemia, exogenous insulin and insulin analogues should be absorbed very fast and appropriate maximum concentrations should be reached very quickly. METHOD: Overview RESULTS AND CONCLUSIONS: The development of new bolus insulins is focused on improved pharmacokinetic and pharmacodynamic properties...
December 2016: MMW Fortschritte der Medizin
https://www.readbyqxmd.com/read/27933555/pharmacist-s-comprehensive-geriatric-assessment-introduction-and-evaluation-at-elderly-patient-admission
#16
Faiza Rhalimi, Mounir Rhalimi, Alain Rauss
BACKGROUND: The role of the clinical pharmacist within the healthcare system remains unclear. OBJECTIVE: Our objective was to describe a pharmacist's comprehensive geriatric assessment (pCGA) at admission of elderly patients and to assess its relevance in terms of medication compliance and pharmacist interventions (PIs). METHODS: We conducted a prospective interventional study over 29 months in a 34-bed medical/rehabilitation geriatric ward in a French geriatric hospital...
December 8, 2016: Drugs—Real World Outcomes
https://www.readbyqxmd.com/read/27933456/penicillin-v-acylases-from-gram-negative-bacteria-degrade-n-acylhomoserine-lactones-and-attenuate-virulence-in-pseudomonas-aeruginosa
#17
Avinash Vellore Sunder, Putri Dwi Utari, Sureshkumar Ramasamy, Ronald van Merkerk, Wim Quax, Archana Pundle
Virulence pathways in gram-negative pathogenic bacteria are regulated by quorum sensing mechanisms, through the production and sensing of N-acylhomoserine lactone (AHL) signal molecules. Enzymatic degradation of AHLs leading to attenuation of virulence (quorum quenching) could pave the way for the development of new antibacterials. Penicillin V acylases (PVAs) belong to the Ntn hydrolase superfamily, together with AHL acylases. PVAs are exploited widely in the pharmaceutical industry, but their role in the natural physiology of their native microbes is not clearly understood...
December 8, 2016: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/27933140/mitigating-pharmaceutical-waste-exposures-policy-and-program-considerations
#18
EDITORIAL
Eric D Amster
Pharmaceutical disposal and the environmental fate of medication metabolites directly impacts the public's health in two significant ways: accidental medication ingestion of pharmaceuticals that were not disposed of properly results in inadvertent toxicity; and environmental health consequences of pharmaceuticals that were inappropriately disposed and which contaminate municipal water supply. In reviewing the effectiveness of medication disposal policy globally, it is crucial to not only determine which policies are effective but also to assess why they are effective...
2016: Israel Journal of Health Policy Research
https://www.readbyqxmd.com/read/27932865/statistical-modeling-methods-to-analyze-the-impacts-of-multiunit-process-variability-on-critical-quality-attributes-of-chinese-herbal-medicine-tablets
#19
Fei Sun, Bing Xu, Yi Zhang, Shengyun Dai, Chan Yang, Xianglong Cui, Xinyuan Shi, Yanjiang Qiao
The quality of Chinese herbal medicine tablets suffers from batch-to-batch variability due to a lack of manufacturing process understanding. In this paper, the Panax notoginseng saponins (PNS) immediate release tablet was taken as the research subject. By defining the dissolution of five active pharmaceutical ingredients and the tablet tensile strength as critical quality attributes (CQAs), influences of both the manipulated process parameters introduced by an orthogonal experiment design and the intermediate granules' properties on the CQAs were fully investigated by different chemometric methods, such as the partial least squares, the orthogonal projection to latent structures, and the multiblock partial least squares (MBPLS)...
2016: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/27932834/pharmaceuticals-antibiotics-and-vegetarians
#20
D J Smith, R A Ratansi, E Mann, J Russell, A Kanatas
No abstract text is available yet for this article.
December 9, 2016: British Dental Journal
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