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https://www.readbyqxmd.com/read/28221039/polycyclic-aromatic-hydrocarbons-via-iron-iii-catalyzed-carbonyl-olefin-metathesis
#1
Christopher C McAtee, Paul S Riehl, Corinna S Schindler
Polycyclic aromatic hydrocarbons are important structural motifs in organic chemistry, pharmaceutical chemistry, and materials science. The development of a new synthetic strategy toward these compounds is described based on the design principle of iron(III)-catalyzed carbonyl-olefin metathesis reactions. This approach is characterized by its operational simplicity, high functional group compatibility, and regioselectivity while relying on FeCl3 as an environmentally benign, earth-abundant metal catalyst. Experimental evidence for oxetanes as reactive intermediates in the catalytic carbonyl-olefin ring-closing metathesis has been obtained...
February 21, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28205403/functionalized-calix-4-arenes-as-potential-therapeutic-agents
#2
Muhammad Moazzam Naseer, Mukhtiar Ahmed, Shahid Hameed
Calixarenes, composed of phenolic units linked by methylene bridges at the 2,6-positions, represent a versatile class of macrocyclic compounds in supramolecular chemistry that can host small molecules or ions in their well-defined hydrophobic cavities. In recent years, it has been recognized that this class of compounds has the potential to serve as platform for the design of biological active compounds. Therefore, the calixarenes functionalized with different pharmacophoric groups have been synthesized as target structure by many researchers and were further evaluated for their biological activities...
February 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28205401/computer-aided-drug-design-to-explore-cyclodextrin-therapeutics-and-biomedical-applications
#3
Azizeh Abdolmaleki, Fatemeh Ghasemi, Jahan B Ghasemi
Cyclodextrin (CD) is a subset of the macrocyclic structural class, which is an important class of small organic agents that are useful functional excipients. They have wide range application possibilities in different fields of sciences such as material preparation, medicine, analytical chemistry, and separation processes. They are used widely in pharmaceutical formulations and drug delivery for increasing the water solubility of low soluble drugs and drug candidates. Due to the ring structure, they behave differently than smaller molecules and may be capable of hitting new classes of targets...
February 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28199101/fungal-identification-using-molecular-tools-a-primer-for-the-natural-products-research-community
#4
Huzefa A Raja, Andrew N Miller, Cedric J Pearce, Nicholas H Oberlies
Fungi are morphologically, ecologically, metabolically, and phylogenetically diverse. They are known to produce numerous bioactive molecules, which makes them very useful for natural products researchers in their pursuit of discovering new chemical diversity with agricultural, industrial, and pharmaceutical applications. Despite their importance in natural products chemistry, identification of fungi remains a daunting task for chemists, especially those who do not work with a trained mycologist. The purpose of this review is to update natural products researchers about the tools available for molecular identification of fungi...
February 15, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28192909/local-rank-deficiency-caused-problems-in-analyzing-chemical-data
#5
Mahsa Akbari Lakeh, Róbert Rajkó, Hamid Abdollahi
Multivariate curve resolution (MCR) is a powerful methodology for analyzing chemical data in different application fields such as pharmaceutical analysis, agriculture, food chemistry, environment, and industrial and clinical chemistry. However, MCR results are often complicated by rotational ambiguity, meaning that there is a range of feasible solutions that fulfill the constraints and explain equally well the observed experimental data. Constraints determine the properties of resolved profiles in MCR methods by enforcing different assumptions on data...
February 3, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/28182958/positioning-metal-organic-framework-nanoparticles-within-the-context-of-drug-delivery-a-comparison-with-mesoporous-silica-nanoparticles-and-dendrimers
#6
Stefan Wuttke, Marjorie Lismont, Alberto Escudero, Bunyarat Rungtaweevoranit, Wolfgang J Parak
Nanotechnology enables the creation of delivery vehicles able to overcome physiologically imposed barriers, allowing new approaches for reducing the unwanted side effects of systemic delivery of drug, increasing targeting efficiency and so improving therapy efficacy. Owing to the considerable advances in material sciences and pharmaceutics, a broad range of different inorganic or organic drug nanocarriers have been developed. Furthermore, researchers have shown that the combination of inorganic and organic chemistries in one single material, named metal-organic framework (MOF), offers structural designability at the molecular level together with tunable porosity and chemical functionalisability...
January 30, 2017: Biomaterials
https://www.readbyqxmd.com/read/28181828/synthesis-of-sericin-based-conjugates-by-click-chemistry-enhancement-of-sunitinib-bioavailability-and-cell-membrane-permeation
#7
Luca Scrivano, Domenico Iacopetta, Maria Stefania Sinicropi, Carmela Saturnino, Pasquale Longo, Ortensia Ilaria Parisi, Francesco Puoci
Sericin is a natural protein that has been used in biomedical and pharmaceutical fields as raw material for polypeptide-based drug delivery systems (DDSs). In this paper, it has been employed as pharmaceutical biopolymer for the production of sunitinib-polypeptide conjugate. The synthesis has been carried out by simple click reaction in water, using the redox couple l-ascorbic acid/hydrogen peroxide as a free radical grafting initiator. The bioconjugate molecular weight (50 kDa < Mw < 75 kDa) was obtained by SDS-PAGE, while the spectroscopic characteristics have been studied in order to reveal the presence of grafted sunitinib...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28177013/recent-developments-in-sulfur-carbon-bond-formation-reaction-involving-thiosulfates
#8
Zongjun Qiao, Xuefeng Jiang
Sulfur-carbon bond construction has gained great attention recently since sulfur-containing organic molecules serve important functions in the pharmaceutical industry, agrochemistry, food chemistry, and materials science. Diverse sulfur sources have been developed over the past few decades, in which thiosulfates showed unique properties in many transformations. In this Perspective, we summarized recent research on sulfur-carbon bond formation involving thiosulfates.
February 8, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28171830/a-review-on-antioxidant-potential-of-bioactive-heterocycle-benzofuran-natural-and-synthetic-derivatives
#9
REVIEW
Karam Chand, Rajeshwari, Asha Hiremathad, Mahak Singh, M Amelia Santos, Rangappa S Keri
The majority of heterocycle compounds and typically common heterocycle fragments present in most pharmaceuticals currently marketed, alongside with their intrinsic versatility and unique physicochemical properties, have poised them as true cornerstones of medicinal chemistry. In this context, oxygen heterocycles exhibit diverse biological and pharmacological activities due in part to the similarities with many natural and synthetic molecules with known biological activity. Among oxygen containing heterocycles, benzofuran (synthetic and natural isolated) and its derivatives have attracted medicinal chemists and pharmacologists due to their pronounced biological activities and their potential applications as pharmacological agents such as antioxidant, antitumor, antiplatelet, antimalarial, antiinflammatory, antidepressant and anticonvulsant properties...
November 18, 2016: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28168709/recent-trends-and-applications-in-liquid-phase-chromatography-enantioseparation-of-atropisomers
#10
REVIEW
Paola Peluso, Victor Mamane, Emmanuel Aubert, Sergio Cossu
The term Atropisomerism defines a type of enantiomerism that arises from hindered rotation around an axis that makes two rotational isomers enantiomers. Atropisomeric compounds are present in nature, being important building blocks of many biologically active compounds. Atropisomers have been extensively studied in environmental and toxicological chemistry and, in particular, separating them has become a need in specific fields as organic synthesis and pharmaceutical research. High-performance liquid chromatography has been fruitfully applied in this context, and, despite HPLC separation on chiral stationary phase (CSP) is considered as mature technology nowadays, in the last years several advancements and applications contributed to study compounds where axial chirality is of utmost importance...
February 6, 2017: Electrophoresis
https://www.readbyqxmd.com/read/28164761/mitogen-activated-protein-kinase-mapk-interacting-kinases-1-and-2-mnk1-and-mnk2-as-targets-for-cancer-therapy-recent-progress-in-the-development-of-mnk-inhibitors
#11
Agnieszka Dreas, Maciej Mikulski, Mariusz Milik, Charles-Henry Fabritius, Krzysztof Brzózka, Tomasz Rzymski
BACKGROUND: MNK1 and MNK2 are MAP kinase-interacting serine/threonine kinases, which are activated by RAS and MAPK signaling pathways and are involved in regulation of protein translation. Both kinases phosphorylate translation initiation factor eIF4E on a conserved serine 209. Overactivated eIF4E can act as an oncogene and contribute to the transformation both in vitro and in vivo and is highly expressed in diverse types of cancer. Interestingly, knockout mice that lack both Mnk1 and Mnk2 do not have any apparent phenotype...
February 3, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28153578/improving-drug-like-properties-of-insulin-and-glp-1-via-molecule-design-and-formulation-and-improving-diabetes-management-with-device-drug-delivery
#12
REVIEW
Sergei Pechenov, Himanshu Bhattacharjee, Daniel Yin, Sachin Mittal, Anand Subramony
There is an increased incidence of diabetes worldwide. The discovery of insulin revolutionized the management of diabetes, the revelation of glucagon-like peptide -1 (GLP-1) and introduction of GLP-1 mimetics to clinical practice was another breakthrough. Continued translational research resulted in better understanding of diabetes, which, in combination with cutting-edge biology, chemistry, and pharmaceutical tools, have allowed for the development of safer, more effective and convenient insulins and GLP-1s...
January 30, 2017: Advanced Drug Delivery Reviews
https://www.readbyqxmd.com/read/28150944/halogen-mediated-conversion-of-hydrocarbons-to-commodities
#13
Ronghe Lin, Amol P Amrute, Javier Pérez-Ramírez
Halogen chemistry plays a central role in the industrial manufacture of various important chemicals, pharmaceuticals, and polymers. It involves the reaction of halogens or halides with hydrocarbons, leading to intermediate compounds which are readily converted to valuable commodities. These transformations, predominantly mediated by heterogeneous catalysts, have long been successfully applied in the production of polymers. Recent discoveries of abundant conventional and unconventional natural gas reserves have revitalized strong interest in these processes as the most cost-effective gas-to-liquid technologies...
February 2, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28146112/second-international-electronic-conference-on-medicinal-chemistry-ecmc-2
#14
Annie Mayence, Jean Jacques Vanden Eynde
The second International Electronic Conference on Medicinal Chemistry, organized and sponsored by the publisher MDPI AG and the Journal Pharmaceuticals, took place in November 2016 on the SciForum website (www.sciforum.net/conference/ecmc-12). More than 150 authors from 22 countries participated in the event. Selected works presented during the scientific meeting are disclosed in this report.
January 31, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28145825/emerging-technologies-in-solid-drug-delivery-an-interview-with-nadia-passerini
#15
Nadia Passerini
Nadia Passerini is interviewed by Hannah Makin, Commission Editor. Nadia Passerini is Associate Professor of Pharmaceutical Technology at the University of Bologna (Bologna, Italy). She obtained the degree in Pharmaceutical Chemistry and Technology at the University of Bologna in 1992 and the PhD in Pharmaceutical Science in 1997. Her research focuses on the study of drug delivery systems, developing new technologies and new apparatus for the production of solid dosage forms (microparticles, granules and tablets), which can optimize the bioavailability of drugs according to the specific needs of the therapy...
January 2017: Therapeutic Delivery
https://www.readbyqxmd.com/read/28138514/the-thermodynamic-scale-of-inorganic-crystalline-metastability
#16
Wenhao Sun, Stephen T Dacek, Shyue Ping Ong, Geoffroy Hautier, Anubhav Jain, William D Richards, Anthony C Gamst, Kristin A Persson, Gerbrand Ceder
The space of metastable materials offers promising new design opportunities for next-generation technological materials, such as complex oxides, semiconductors, pharmaceuticals, steels, and beyond. Although metastable phases are ubiquitous in both nature and technology, only a heuristic understanding of their underlying thermodynamics exists. We report a large-scale data-mining study of the Materials Project, a high-throughput database of density functional theory-calculated energetics of Inorganic Crystal Structure Database structures, to explicitly quantify the thermodynamic scale of metastability for 29,902 observed inorganic crystalline phases...
November 2016: Science Advances
https://www.readbyqxmd.com/read/28131588/simplified-solid-phase-extraction-procedure-combined-with-liquid-chromatography-tandem-mass-spectrometry-for-multiresidue-assessment-of-pharmaceutical-compounds-in-environmental-liquid-samples
#17
C Afonso-Olivares, T Čadková, Z Sosa-Ferrera, J J Santana-Rodríguez, L Nováková
To follow the twelve "green analytical chemistry" (GAC) principles, it is necessary to continuously develop analytical extraction and determination methodologies to assess the presence of micropollutants, such as pharmaceuticals, in environmental samples. A reduction in the analysis time and solvent quantity, which is one of the GAC principles, has been achieved through a simplified solid-phase extraction (SPE) procedure combined with high-performance liquid chromatography-tandem mass spectrometry (LC-MS/MS) for the determination of twenty-three pharmaceuticals in liquid environmental samples using N-vinylpyrrolidone-divinylbenzene copolymer (OASIS HLB) cartridges...
March 3, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28128923/base-mediated-hydroamination-of-alkynes
#18
Monika Patel, Rakesh K Saunthwal, Akhilesh K Verma
Inter- or intramolecular hydroamination reactions are a paradigmatic example of modern sustainable organic chemistry, as they are a catalytic, 100% atom-economical, and waste-free process of fundamental simplicity in which an amine is added to an alkyne substrate. Many enamines are found in many natural and synthetic compounds possessing interesting physiological and biological activities. The development of synthetic protocols for such molecules and their transformation is a persistent research topic in pharmaceutical and organic chemistry...
January 27, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28125212/biological-activity-of-ionic-liquids-and-their-application-in-pharmaceutics-and-medicine
#19
Ksenia S Egorova, Evgeniy G Gordeev, Valentine P Ananikov
Ionic liquids are remarkable chemical compounds, which find applications in many areas of modern science. Because of their highly tunable nature and exceptional properties, ionic liquids have become essential players in the fields of synthesis and catalysis, extraction, electrochemistry, analytics, biotechnology, etc. Apart from physical and chemical features of ionic liquids, their high biological activity has been attracting significant attention from biochemists, ecologists, and medical scientists. This Review is dedicated to biological activities of ionic liquids, with a special emphasis on their potential employment in pharmaceutics and medicine...
January 26, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28116390/recent-progress-in-cellulose-nanocrystals-sources-and-production
#20
REVIEW
Djalal Trache, M Hazwan Hussin, M K Mohamad Haafiz, Vijay Kumar Thakur
Cellulose nanocrystals, a class of fascinating bio-based nanoscale materials, have received a tremendous amount of interest both in industry and academia owing to its unique structural features and impressive physicochemical properties such as biocompatibility, biodegradability, renewability, low density, adaptable surface chemistry, optical transparency, and improved mechanical properties. This nanomaterial is a promising candidate for applications in fields such as biomedical, pharmaceuticals, electronics, barrier films, nanocomposites, membranes, supercapacitors, etc...
January 24, 2017: Nanoscale
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