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Pharmaceutical chemistry

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https://www.readbyqxmd.com/read/28724346/biosensing-technologies-for-therapeutic-drug-monitoring
#1
Anna Meneghello, Stefano Tartaggia, Maria Domenica Alvau, Federico Polo, Giuseppe Toffoli
Therapeutic drug monitoring (TDM) is the clinical practice of measuring pharmaceutical drug concentrations in patients' biofluids at designated intervals to allow a close and timely control of their dosage. This practice allows for rapid medical intervention in case of toxicity-related issues and/or adjustment of dosage to better fit the therapeutic demand. Currently, TDM is performed in centralized laboratories employing instruments, such as immunoassay analyzers and mass spectrometers that can be run only by trained personnel...
July 20, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28718642/predictive-model-for-site-selective-aryl-and-heteroaryl-c-h-functionalization-via-organic-photoredox-catalysis
#2
Kaila A Margrey, Joshua B McManus, Simone Bonazzi, Frederic Zecri, David A Nicewicz
Direct C-H functionalization of aromatic compounds is a useful synthetic strategy that has garnered much attention due to its application to pharmaceuticals, agrochemicals, and late stage functionalization reactions on complex molecules. Based on previous methods disclosed by our lab, we sought to develop a predictive model for site selectivity and extend this aryl functionalization chemistry to a selected set of heteroaromatic systems commonly used in the pharmaceutical industry. Using electron density calculations, we were able to predict site selectivity of direct C-H functionalization in a number of heterocycles and identify general trends observed across heterocycle classes...
July 18, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28718326/cns-anticancer-drug-discovery-and-development-2016-conference-insights
#3
Victor A Levin, Lauren E Abrey, Timothy P Heffron, Peter J Tonge, Arvin C Dar, William A Weiss, James M Gallo
CNS Anticancer Drug Discovery and Development November 2016, AZ, USA The 2016 second CNS Anticancer Drug Discovery and Development Conference addressed diverse viewpoints about why new drug discovery/development focused on CNS cancers has been sorely lacking. Despite more than 70,000 individuals in the USA being diagnosed with a primary brain malignancy and 151,669-286,486 suffering from metastatic CNS cancer, in 1999, temozolomide was the last drug approved by the US FDA as an anticancer agent for high-grade gliomas...
July 18, 2017: CNS Oncology
https://www.readbyqxmd.com/read/28717021/genetic-and-metabolic-engineering-in-diatoms
#4
REVIEW
Weichao Huang, Fayza Daboussi
Diatoms have attracted considerable attention due to their success in diverse environmental conditions, which probably is a consequence of their complex origins. Studies of their metabolism will provide insight into their adaptation capacity and are a prerequisite for metabolic engineering. Several years of investigation have led to the development of the genome engineering tools required for such studies, and a profusion of appropriate tools is now available for exploring and exploiting the metabolism of these organisms...
September 5, 2017: Philosophical Transactions of the Royal Society of London. Series B, Biological Sciences
https://www.readbyqxmd.com/read/28716314/safety-and-efficacy-of-ebselen-for-the-prevention-of-noise-induced-hearing-loss-a-randomised-double-blind-placebo-controlled-phase-2-trial
#5
Jonathan Kil, Edward Lobarinas, Christopher Spankovich, Scott K Griffiths, Patrick J Antonelli, Eric D Lynch, Colleen G Le Prell
BACKGROUND: Noise-induced hearing loss is a leading cause of occupational and recreational injury and disease, and a major determinant of age-related hearing loss. No therapeutic agent has been approved for the prevention or treatment of this disorder. In animal models, glutathione peroxidase 1 (GPx1) activity is reduced after acute noise exposure. Ebselen, a novel GPx1 mimic, has been shown to reduce both temporary and permanent noise-induced hearing loss in preclinical studies. We assessed the safety and efficacy of ebselen for the prevention of noise-induced hearing loss in young adults in a phase 2 clinical trial...
July 14, 2017: Lancet
https://www.readbyqxmd.com/read/28716104/evaluating-the-potential-of-gold-silver-and-silica-nanoparticles-to-saturate-mononuclear-phagocytic-system-tissues-under-repeat-dosing-conditions
#6
James L Weaver, Grainne A Tobin, Taylor Ingle, Simona Bancos, David Stevens, Rodney Rouse, Kristina E Howard, David Goodwin, Alan Knapton, Xiaohong Li, Katherine Shea, Sharron Stewart, Lin Xu, Peter L Goering, Qin Zhang, Paul C Howard, Jessie Collins, Saeed Khan, Kidon Sung, Katherine M Tyner
BACKGROUND: As nanoparticles (NPs) become more prevalent in the pharmaceutical industry, questions have arisen from both industry and regulatory stakeholders about the long term effects of these materials. This study was designed to evaluate whether gold (10 nm), silver (50 nm), or silica (10 nm) nanoparticles administered intravenously to mice for up to 8 weeks at doses known to be sub-toxic (non-toxic at single acute or repeat dosing levels) and clinically relevant could produce significant bioaccumulation in liver and spleen macrophages...
July 17, 2017: Particle and Fibre Toxicology
https://www.readbyqxmd.com/read/28711855/exploiting-and-engineering-hemoproteins-for-abiological-carbene-and-nitrene-transfer-reactions
#7
REVIEW
Oliver F Brandenberg, Rudi Fasan, Frances H Arnold
The surge in reports of heme-dependent proteins as catalysts for abiotic, synthetically valuable carbene and nitrene transfer reactions dramatically illustrates the evolvability of the protein world and our nascent ability to exploit that for new enzyme chemistry. We highlight the latest additions to the hemoprotein-catalyzed reaction repertoire (including carbene Si-H and C-H insertions, Doyle-Kirmse reactions, aldehyde olefinations, azide-to-aldehyde conversions, and intermolecular nitrene C-H insertion) and show how different hemoprotein scaffolds offer varied reactivity and selectivity...
July 13, 2017: Current Opinion in Biotechnology
https://www.readbyqxmd.com/read/28704396/phenotypic-chemical-and-functional-characterization-of-cyclic-nucleotide-phosphodiesterase-4-pde4-as-a-potential-anthelmintic-drug-target
#8
Thavy Long, Liliana Rojo-Arreola, Da Shi, Nelly El-Sakkary, Kurt Jarnagin, Fernando Rock, Maliwan Meewan, Alberto A Rascón, Lin Lin, Katherine A Cunningham, George A Lemieux, Larissa Podust, Ruben Abagyan, Kaveh Ashrafi, James H McKerrow, Conor R Caffrey
BACKGROUND: Reliance on just one drug to treat the prevalent tropical disease, schistosomiasis, spurs the search for new drugs and drug targets. Inhibitors of human cyclic nucleotide phosphodiesterases (huPDEs), including PDE4, are under development as novel drugs to treat a range of chronic indications including asthma, chronic obstructive pulmonary disease and Alzheimer's disease. One class of huPDE4 inhibitors that have yielded marketed drugs is the benzoxaboroles (Anacor Pharmaceuticals)...
July 13, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/28702645/a-perspective-can-copper-complexes-be-developed-as-a-novel-class-of-therapeutics
#9
Mohamed Wehbe, Ada W Y Leung, Michael J Abrams, Chris Orvig, Marcel B Bally
Although copper-ligand complexes appear to be promising as a new class of therapeutics, other than the family of copper(ii) coordination compounds referred to as casiopeínas these compounds have yet to reach the clinic for human use. The pharmaceutical challenges associated with developing copper-based therapeutics will be presented in this article along with a discussion of the potential for high-throughput chemistry, computer-aided drug design, and nanotechnology to address the development of this important class of drug candidates...
July 12, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28687508/a-framework-for-the-targeted-selection-of-herbs-with-similar-efficacy-by-exploiting-drug-repositioning-technique-and-curated-biomedical-knowledge
#10
Sang-Jun Yea, Bu-Yeo Kim, Chul Kim, Mun Yong Yi
ETHNO PHARMACOLOGICAL RELEVANCE: Plants have been the most important natural resources for traditional medicine and for the modern pharmaceutical industry. They have been in demand in regards to finding alternative medicinal herbs with similar efficacy. Due to the very low probability of discovering useful compounds by random screening, researchers have advocated for using targeted selection approaches. Furthermore, because drug repositioning can speed up the process of drug development, an integrated technique that exploits chemical, genetic, and disease information has been recently developed...
July 5, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28680362/medical-biochemistry-as-subdiscipline-of-laboratory-medicine-in-serbia
#11
Snežana Jovičić, Nada Majkić-Singh
Medical biochemistry is the usual name for clinical biochemistry or clinical chemistry in Serbia, and medical biochemist is the official name for the clinical chemist (or clinical biochemist). This is the largest sub-discipline of the laboratory medicine in Serbia. It includes all aspects of clinical chemistry, and also laboratory hematology with coagulation, immunology, etc. Medical biochemistry laboratories in Serbia and medical biochemists as a profession are part of Health Care System and their activities are regulated through: the Health Care Law and rules issued by the Chamber of Medical Biochemists of Serbia...
April 2017: Journal of Medical Biochemistry
https://www.readbyqxmd.com/read/28676386/prodrugs-in-medicinal-chemistry-and-enzyme-prodrug-therapies
#12
Raoul Walther, Jarkko Rautio, Alexander N Zelikin
Prodrugs are cunning derivatives of therapeutic agents designed to improve the pharmacokinetics profile of the drug. Within a prodrug, pharmacological activity of the drug is masked and is recovered within the human body upon bioconversion of the prodrug, a process that is typically mediated by enzymes. This concept is highly successful and a significant fraction of marketed therapeutic formulations is based on prodrugs. An advanced subset of prodrugs can be engineered such as to achieve site-specific bioconversion of the prodrug - to comprise the highly advantageous "enzyme prodrug therapy", EPT...
July 1, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28676003/synthesis-structural-characterization-and-antinociceptive-activities-of-new-arylated-quinolines-via-suzuki-miyaura-cross-coupling-reaction
#13
Malik Aman Ullah, Muhammad Adeel, Muhammad N Tahir, Abdur Rauf, Muhammad Akram, Taibi Ben Hadda, Yahia N Mabkhot, Naveed Muhammad, Fehmida Naseer, Mohammad S Mubarak
Backgorund: The quinoline ring system is one of the most commonly encountered heterocycles in medicinal chemistry, due to the pharmaceutical and medicinal uses of derivatives containing this ring. These quinoline-based compounds have remarkable biological activity, as they are employed as antimalarial, antibacterial, antifungal, and antitumor agents. The quinoline nucleus can be synthesized by various traditional methods such as the Skraup reaction, Friedlaender synthesis, Combes quinoline synthesis, Larock quinoline synthesis, among others...
July 4, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28675773/a-polymer-chemistry-point-of-view-on-mucoadhesion-and-mucopenetration
#14
REVIEW
Philipp Schattling, Essi Taipaleenmäki, Yan Zhang, Brigitte Städler
Although oral is the preferred route of administration of pharmaceutical formulations, the long-standing challenge for medically active compounds to efficiently cross the mucus layer barrier limits its wider applicability. Efforts in nanomedicine to overcome this hurdle consider mucoadhesive and mucopenetrating drug carriers by selectively designing (macromolecular) building blocks. This review highlights and critically discusses recent strategies developed in this context including poly(ethylene glycol)-based modifications, cationic and thiolated polymers, as well as particles with high charge density, zeta-potential shifting ability, or mucolytic properties...
July 4, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28672096/metabolomic-tools-to-assess-the-chemistry-and-bioactivity-of-endophytic-aspergillus-strain
#15
A F Tawfike, R Tate, G Abbott, L Young, C Viegelmann, M Schumacher, M Diederich, R A Edrada-Ebel
Endophytic fungi associated with medicinal plants are a potential source of novel chemistry and biology that may find applications as pharmaceutical and agrochemical drugs. In this study, a combination of metabolomics and bioactivity-guided approaches were employed to isolate anticancer secondary metabolites from an endophytic Aspergillus aculeatus. The endophyte was isolated from the Egyptian medicinal plant Terminalia laxiflora and identified using molecular biological methods. Metabolomics and dereplication studies were accomplished by utilizing the MZmine software coupled with the universal Dictionary of Natural Products database...
July 3, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28671733/centennial-anniversary-of-mannich-s-report-on-the-formation-of-%C3%AE-amino-ketones-in-the-archiv-der-pharmazie
#16
EDITORIAL
Andreas Link
In order to commemorate Carl Mannich's achievement with many implications in the fields of drug design and synthesis, stability of pharmaceutical preparations, and natural product chemistry, we invited researchers to submit their work related to Mannich's pioneering article at the occasion of its centennial anniversary to the Archiv der Pharmazie - where else?
July 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28670474/on-the-bridge-over-the-translational-valley-of-death-interview-with-per-i-arvidsson
#17
Per I Arvidsson
Per I Arvidsson speaks to Francesca Lake, Managing Editor: Per received his PhD in organic chemistry from Gothenburg University (Sweden) in 1999, where he continued as a lecturer for a short time. Following 2 years at the ETH Zurich (Switzerland) as a postdoctoral fellow, he went on to establish an independent research group at the Department of Biochemistry and Organic Chemistry at Uppsala University (Sweden). In 2006, he joined AstraZeneca R&D Södertälje (Sweden). After 1-year in-house training for future leaders in drug discovery and development, he became team leader in Medicinal Chemistry in 2007...
June 2017: Future Science OA
https://www.readbyqxmd.com/read/28667106/discovery-of-lysine-hydroxylases-in-the-clavaminic-acid-synthase-like-superfamily-for-efficient-hydroxylysine-bioproduction
#18
Ryotaro Hara, Kai Yamagata, Ryoma Miyake, Hiroshi Kawabata, Hisatoshi Uehara, Kuniki Kino
Hydroxylation via C--H bond activation in the absence of any harmful oxidizing reagents is technically difficult in modern chemistry. In this work, we attempted to generate pharmaceutically important hydroxylysine from readily available l-lysine with l-lysine hydroxylases from diverse microorganisms. Clavaminic acid synthase-like superfamily gene mining and phylogenetic analysis led to the discovery of six biocatalysts-two l-lysine 3S-hydroxylases and four l-lysine 4R-hydroxylases. The latter of which partially matched known hydroxylases...
June 30, 2017: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/28648380/privileged-electrophile-sensors-a-resource-for-covalent-drug-development
#19
REVIEW
Marcus John Curtis Long, Yimon Aye
This Perspective delineates how redox signaling affects the activity of specific enzyme isoforms and how this property may be harnessed for rational drug design. Covalent drugs have resurged in recent years and several reports have extolled the general virtues of developing irreversible inhibitors. Indeed, many modern pharmaceuticals contain electrophilic appendages. Several invoke a warhead that hijacks active-site nucleophiles whereas others take advantage of spectator nucleophilic side chains that do not participate in enzymatic chemistry, but are poised to bind/react with electrophiles...
July 20, 2017: Cell Chemical Biology
https://www.readbyqxmd.com/read/28648054/practical-singly-and-doubly-electrophilic-aminating-agents-a-new-more-sustainable-platform-for-carbon-nitrogen-bond-formation
#20
Padmanabha V Kattamuri, Jun Yin, Surached Siriwongsup, Doo-Hyun Kwon, Daniel H Ess, Qun Li, Guigen Li, Muhammed Yousufuddin, Paul F Richardson, Scott C Sutton, László Kürti
Given the importance of amines in a large number of biologically active natural products, active pharmaceutical ingredients, agrochemicals, and functional materials, the development of efficient C-N bond-forming methods with wide substrate scope continues to be at the frontier of research in synthetic organic chemistry. Here, we present a general and fundamentally new synthetic approach for the direct, transition-metal-free preparation of symmetrical and unsymmetrical diaryl-, arylalkyl-, and dialkylamines that relies on the facile single or double addition of readily available C-nucleophiles to the nitrogen atom of bench-stable electrophilic aminating agents...
July 13, 2017: Journal of the American Chemical Society
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