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Pharmaceutical chemistry

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https://www.readbyqxmd.com/read/28101455/pharmaceutical-cocrystals-regulatory-and-strategic-aspects-design-and-development
#1
REVIEW
Dipak Dilip Gadade, Sanjay Sudhakar Pekamwar
Cocrystal is a concept of the supramolecular chemistry which is gaining the extensive interest of researchers from pharmaceutical and chemical sciences and of drug regulatory agencies. The prominent reason of which is its ability to modify physicochemical properties of active pharmaceutical ingredients. During the development of the pharmaceutical product, formulators have to optimize the physicochemical properties of active pharmaceutical ingredients. Pharmaceutical cocrystals can be employed to improve vital physicochemical characteristics of a drug, including solubility, dissolution, bioavailability and stability of pharmaceutical compounds while maintaining its therapeutic activity...
December 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28093829/unprecedented-access-to-%C3%AF-arylated-selenophenes-via-palladium-catalysed-direct-arylation
#2
Aymen Skhiri, Ridha Ben Salem, Jean-Francois Soulé, Henri Doucet
Several methods allow the access to a-arylated selenophenes; whereas the synthesis of b-arylated selenophenes remains very challenging. We demonstrated that the Pd-catalysed coupling of benzenesulfonyl chlorides with selenophenes affords regiospecifically the b-arylated selenophenes. The reaction proceeds with easily accessible catalyst, base and substrates, and tolerates a variety of substituents both on the benzene and selenophene moieties. This transformation allows the programmed synthesis of polyarylated selenophenes with potential applications in pharmaceutical and material chemistry, as the installation of aryl groups at the desired positions can be achieved...
January 17, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28092854/biopharmaceutical-characterization-of-praziquantel-cocrystals-and-cyclodextrin-complexes-prepared-by-grinding
#3
Martina Cugovčan, Jasna Jablan, Jasmina Lovrić, Dominik Cinčić, Nives Galić, Mario Jug
Mechanochemical activation using several different co-grinding additives was applied as a green chemistry approach to improve physiochemical and biopharmaceutical properties of praziquantel (PZQ). Liquid assisted grinding with an equimolar amount of citric acid (CA), malic acid (MA), salicylic acid (SA) and tartaric acid (TA) gained in cocrystal formation, which all showed pH-dependent solubility and dissolution rate. However, the most soluble cocrystal of PZQ with MA was chemically unstable, as seen during the stability testing...
January 10, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/28088572/bcs-class-iv-drugs-highly-notorious-candidates-for-formulation-development
#4
REVIEW
Rohan Ghadi, Neha Dand
BCS class IV drugs (e.g., amphotericin B, furosemide, acetazolamide, ritonavir, paclitaxel) exhibit many characteristics that are problematic for effective oral and per oral delivery. Some of the problems associated include low aqueous solubility, poor permeability, erratic and poor absorption, inter and intra subject variability and significant positive food effect which leads to low and variable bioavailability. Also, most of the class IV drugs are substrate for P-glycoprotein (low permeability) and substrate for CYP3A4 (extensive pre systemic metabolism) which further potentiates the problem of poor therapeutic potential of these drugs...
January 11, 2017: Journal of Controlled Release: Official Journal of the Controlled Release Society
https://www.readbyqxmd.com/read/28087127/the-route-from-problem-to-solution-in-multistep-continuous-flow-synthesis-of-pharmaceutical-compounds
#5
Péter Bana, Róbert Örkényi, Klára Lövei, Ágnes Lakó, György István Túrós, János Éles, Ferenc Faigl, István Greiner
Recent advances in the field of continuous flow chemistry allow the multistep preparation of complex molecules such as APIs (Active Pharmaceutical Ingredients) in a telescoped manner. Numerous examples of laboratory-scale applications are described, which are pointing towards novel manufacturing processes of pharmaceutical compounds, in accordance with recent regulatory, economical and quality guidances. The chemical and technical knowledge gained during these studies is considerable; nevertheless, connecting several individual chemical transformations and the attached analytics and purification holds hidden traps...
December 29, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28078991/vegetable-organosulfur-compounds-and-their-health-promoting-effects
#6
Spyridon A Petropoulos, Francesco Di Gioia, Georgia Ntatsi
BACKGROUND: Trends in modern pharmaceutical science show an increase in demand for new drugs and diet supplements derived from natural products, while during the last decades, great research is conducted regarding the natural compounds and their medicinal and bioactive properties. Organosulfur compounds are present in many plants and their bioactive properties have been used in folk and traditional medicine throughout the centuries. Not until recently, modern science confirmed and revealed the chemical compounds that are responsible for these properties, the chemistry involved in their biosynthesis and the main mechanisms of action...
January 10, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28078952/recent-advances-in-green-nanoparticulate-systems-for-drug-delivery-efficient-delivery-and-safety-concern
#7
Pik-Ling Lam, Wai-Yeung Wong, Zhaoxiang Bian, Chung-Hin Chui, Roberto Gambari
Nanotechnology manipulates therapeutic agents at the nanoscale for the development of nanomedicines. However, there are current concerns over nanomedicines, mainly related to the possible toxicity of nanomaterials used for health medications. Due to their small size, they can enter the human body more readily than larger sized particles. Green chemistry encompasses the green synthesis of drug-loaded nanoparticles by reducing the use of hazardous materials in the synthesis process, thus reducing the adverse health impacts of pharmaceutics...
January 12, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28075527/recent-development-of-the-second-and-third-generation-irreversible-egfr-inhibitors
#8
REVIEW
Weiwei Han, Yongli Du
Recent reports suggested that essential directions for new lung cancer, breast carcinoma therapies, as well as the roomier realm of targeted cancer therapies were provided through targeting the epidermal growth factor receptor (EGFR). Patients who carrying non-small cell lung carcinoma (NSCLC) with activating mutations in EGFR initially respond well to the EGFR inhibitors erlotinib and gefitinib, which were located the active site of the EGFR kinase and designed to act as competitive inhibitors of combining with the ATP...
January 11, 2017: Chemistry & Biodiversity
https://www.readbyqxmd.com/read/28070712/microdialysis-monitoring-in-clinical-traumatic-brain-injury-and-its-role-in-neuroprotective-drug-development
#9
Eric Peter Thelin, Keri L H Carpenter, Peter J Hutchinson, Adel Helmy
Injuries to the central nervous system continue to be vast contributors to morbidity and mortality; specifically, traumatic brain injury (TBI) is the most common cause of death during the first four decades of life. Several modalities are used to monitor patients suffering from TBI in order to prevent detrimental secondary injuries. The microdialysis (MD) technique, introduced during the 1990s, presents the treating physician with a robust monitoring tool for brain chemistry in addition to conventional intracranial pressure monitoring...
January 9, 2017: AAPS Journal
https://www.readbyqxmd.com/read/28068069/re-engineering-extracellular-vesicles-as-smart-nanoscale-therapeutics
#10
James P K Armstrong, Margaret N Holme, Molly M Stevens
In the past decade, extracellular vesicles (EVs) have emerged as a key cell-free strategy for the treatment of a range of pathologies, including cancer, myocardial infarction, and inflammatory diseases. Indeed, the field is rapidly transitioning from promising in vitro reports toward in vivo animal models and early clinical studies. These investigations exploit the high physicochemical stability and biocompatibility of EVs as well as their innate capacity to communicate with cells via signal transduction and membrane fusion...
January 9, 2017: ACS Nano
https://www.readbyqxmd.com/read/28062708/establishment-of-the-in-vivo-efficacy-of-pretargeted-radioimmunotherapy-utilizing-inverse-electron-demand-diels-alder-click-chemistry
#11
Jacob L Houghton, Rosemery Membreno, Dalya Abdel-Atti, Kristen M Cunanan, Sean Carlin, Wolfgang W Scholz, Pat B Zanzonico, Jason S Lewis, Brian M Zeglis
The pretargeting system based on the inverse electron demand Diels-Alder reaction (IEDDA) between trans-cyclooctene (TCO) and tetrazine (Tz) combines the favorable pharmacokinetic properties of radiolabeled small molecules with the affinity and specificity of antibodies. This strategy has proven to be an efficient method for the molecularly targeted delivery of pharmaceuticals, including isotopes for radiological imaging. Despite encouraging results from in vivo PET imaging studies, this promising system has yet to be thoroughly evaluated for pretargeted radioimmunotherapy (PRIT)...
January 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28061690/organophosphorus-xenobiotic-toxicology
#12
John E Casida
Originally, organophosphorus (OP) toxicology consisted of acetylcholinesterase inhibition by insecticides and chemical threat agents acting as phosphorylating agents for serine in the catalytic triad, but this is no longer the case. Other serine hydrolases can be secondary OP targets, depending on the OP structure, and include neuropathy target esterase, lipases, and endocannabinoid hydrolases. The major OP herbicides are glyphosate and glufosinate, which act in plants but not animals to block aromatic amino acid and glutamine biosynthesis, respectively, with safety for crops conferred by their expression of herbicide-tolerant targets and detoxifying enzymes from bacteria...
January 6, 2017: Annual Review of Pharmacology and Toxicology
https://www.readbyqxmd.com/read/28053064/scientific-knowledge-and-technology-animal-experimentation-and-pharmaceutical-development
#13
Lewis B Kinter, Joseph J DeGeorge
Human discovery of pharmacologically active substances is arguably the oldest of the biomedical sciences with origins >3500 years ago. Since ancient times, four major transformations have dramatically impacted pharmaceutical development, each driven by advances in scientific knowledge, technology, and/or regulation: (1) anesthesia, analgesia, and antisepsis; (2) medicinal chemistry; (3) regulatory toxicology; and (4) targeted drug discovery. Animal experimentation in pharmaceutical development is a modern phenomenon dating from the 20th century and enabling several of the four transformations...
December 2016: ILAR Journal
https://www.readbyqxmd.com/read/28052198/contribution-of-surface-chemistry-to-the-shear-thickening-of-silica-nanoparticle-suspensions
#14
Wufang Yang, Yang Wu, Xiaowei Pei, Feng Zhou, Qunji Xue
Shear thickening is a general process crucial for many processed products ranging from food and personal care to pharmaceuticals. Theoretical calculations and mathematical simulations of hydrodynamic interactions and granular-like contacts have proved that contact forces between suspended particles dominate the rheological characteristic of colloidal suspensions. However, relevant experimental studies are very rare. This study was conducted to reveal the influence of nanoparticle (NP) interactions on the rheological behavior of shear-thickening fluids (STFs) by changing the colloidal surface chemistries...
January 17, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/28044422/the-2016-frontiers-in-medicinal-chemistry-conference-in-bonn
#15
Christa E Müller, Dominik Thimm, Karl-Heinz Baringhaus
Pushing the frontiers of medicinal chemistry: Christa Müller, Dominik Thimm, and Karl-Heinz Baringhaus look back at the events of the 2016 Frontiers in Medicinal Chemistry (FiMC) Conference held in Bonn, Germany. The report highlights the themes & talks in the annual conference hosted by the Joint Division of Medicinal Chemistry of the German Pharmaceutical Society (DPhG) and German Chemical Society (GDCh). It is also an invitation to the 2017 conference in Bern, Switzerland this February 12-15.
January 3, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28038491/some-social-aspects-of-discovery-synthesis-and-production-of-cortisone-in-the-1930s-1950s
#16
REVIEW
Daria Jadreškić
A discovery, synthesis and therapeutic application of cortisone present a paradigm for modern translational medicine (Hillier 2007, Saenger 2010), since they represented a joint achievement of discoveries by biochemists, Edward Calvin Kendall and Tadeus Reichstein; large scale synthesis by an industrial chemist, Lewis Hastings Sarett, and therapeutic application by a rheumatologist, Philip Showalter Hench. The goal of translational medicine is to speed up the process between basic research and clinical practice, and to integrate multiple disciplines in order to understand diverse outcomes (Zhang et al...
December 2016: Acta Medico-historica Adriatica: AMHA
https://www.readbyqxmd.com/read/28029135/time-resolved-fluorescence-spectroscopy-and-fluorescence-lifetime-imaging-microscopy-for-characterization-of-dendritic-polymer-nanoparticles-and-applications-in-nanomedicine
#17
REVIEW
Alexander Boreham, Robert Brodwolf, Karolina Walker, Rainer Haag, Ulrike Alexiev
The emerging field of nanomedicine provides new approaches for the diagnosis and treatment of diseases, for symptom relief and for monitoring of disease progression. One route of realizing this approach is through carefully constructed nanoparticles. Due to the small size inherent to the nanoparticles a proper characterization is not trivial. This review highlights the application of time-resolved fluorescence spectroscopy and fluorescence lifetime imaging microscopy (FLIM) for the analysis of nanoparticles, covering aspects ranging from molecular properties to particle detection in tissue samples...
December 24, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28017128/role-of-azoles-in-cancer-prevention-and-treatment-present-and-future-perspectives
#18
Khurshid Ahmad, Mohd Kalim A Khan, Mohammad Hassan Baig, Mohd Imran, Girish Kumar Gupta
Cancer has gradually become one of the leading causes of death worldwide. The incidence of cancer among the population worldwide has increased in an alarming way over the last 2 decades, primarily due to an increasing population of immune-compromised patients and the continuing rise in anti-cancer drug resistance. Azole found privileged structure in medicinal chemistry and pharmaceutical industry and also found very effective against a number of biological targets including antioxidant; antimicrobial, antihelmintic, anticancer, antiviral, anti-parasitic, anti-inflammatory, anti-HIV, and antihypertensive activities...
December 21, 2016: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28013366/teaming-up-synthetic-chemistry-and-histochemistry-for-activity-screening-in-galectin-directed-inhibitor-design
#19
René Roy, Yihong Cao, Herbert Kaltner, Naresh Kottari, Tze Chieh Shiao, Karima Belkhadem, Sabine André, Joachim C Manning, Paul V Murphy, Hans-Joachim Gabius
A hallmark of endogenous lectins is their ability to select a few distinct glycoconjugates as counterreceptors for functional pairing from the natural abundance of cellular glycoproteins and glycolipids. As a consequence, assays to assess inhibition of lectin binding should necessarily come as close as possible to the physiological situation, to characterize an impact of a synthetic compound on biorelevant binding with pharmaceutical perspective. We here introduce in a proof-of-principle manner work with sections of paraffin-embedded tissue (jejunum, epididymis) and labeled adhesion/growth-regulatory galectins, harboring one (galectin-1 and galectin-3) or two (galectin-8) types of lectin domain...
December 24, 2016: Histochemistry and Cell Biology
https://www.readbyqxmd.com/read/28003662/polyanionic-cyclodextrin-induced-supramolecular-nanoparticle
#20
He-Lue Sun, Ying-Ming Zhang, Yong Chen, Yu Liu
Ionizable cyclodextrins have attracted increasing attention in host-guest chemistry and pharmaceutical industry, mainly due to the introduction of favorable electrostatic interactions. The ionizable cyclodextrins could not only enhance its own solubility but also induce oppositely charged guests to form more stable complex. However, the aggregation induced by charged cyclodextrins has rarely been reported. In this work, guided by the concept of molecular-induced aggregation, a series of carboxyl modified cyclodextrins were synthesized via "click" and hydrolysis reaction...
December 2016: Scientific Reports
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