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Pharmaceutical chemistry

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https://www.readbyqxmd.com/read/28524077/highly-stereoselective-synthesis-of-a-compound-collection-based-on-the-bicyclic-scaffolds-of-natural-products
#1
Murali Annamalai, Stanimira Hristeva, Martyna Bielska, Raquel Ortega, Kamal Kumar
Despite the great contribution of natural products in the history of successful drug discovery, there are significant limitations that persuade the pharmaceutical industry to evade natural products in drug discovery research. The extreme scarcity as well as structural complexity of natural products renders their practical synthetic access and further modifications extremely challenging. Although other alternative technologies, particularly combinatorial chemistry, were embraced by the pharmaceutical industry to get quick access to a large number of small molecules with simple frameworks that often lack three-dimensional complexity, hardly any success was achieved in the discovery of lead molecules...
May 18, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28522008/chitosan-chondroitin-sulfate-hydrogels-prepared-in-hmim-hso4-ionic-liquid
#2
Cátia S Nunes, Kessily B Rufato, Paulo R Souza, Elizângela A M S de Almeida, Michael J V da Silva, Débora B Scariot, Celso V Nakamura, Fernanda A Rosa, Alessandro F Martins, Edvani C Muniz
[Hmim][HSO4] ionic liquid (IL) and bio-renewable sources as chitosan (CHT) and chondroitin sulfate (CS) were used to yield hydrogel-based materials (CHT/CS). The use of IL to solubilize both polysaccharides was considered an innovative way based on "green chemistry" principle, aiming the production of CHT/CS blended systems. CHT/CS hydrogels were carried out in homogeneous medium from short dissolution times. The hydrogels were characterized and achieved with excellent stabilities (in the 1.2-10pH range), larger swelling capacities, as well as devoid of cytotoxicity towards the normal VERO and diseased HT29 cells...
August 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28512176/extractables-screening-of-polypropylene-resins-used-in-pharmaceutical-packaging-for-safety-hazards
#3
Dennis Jenke
Pharmaceutical products are packaged in containers so that they can be manufactured, distributed and used. Because extractables from such containers are precursors of leachable impurities in the product, extractables represent potential hazards to user safety. Polypropylene resins are frequently used as materials of construction for packaging of liquid parenteral drug products. Thus extractables profiling of polypropylene resins may be an effective means of hazard identification associated with the resin's safe use...
May 15, 2017: PDA Journal of Pharmaceutical Science and Technology
https://www.readbyqxmd.com/read/28512003/towards-a-sustainable-biobased-industry-highlighting-the-impact-of-extremophiles
#4
REVIEW
Anna Krüger, Christian Schäfers, Carola Schröder, Garabed Antranikian
The transition of the oil-based economy towards a sustainable economy completely relying on biomass as renewable feedstock requires the concerted action of academia, industry, politics and civil society. An interdisciplinary approach of various fields such as microbiology, molecular biology, chemistry, genetics, chemical engineering and agriculture in addition to cross-sectional technologies such as economy, logistics and digitalization is necessary to meet the future global challenges. The genomic era has contributed significantly to the exploitation of naturés biodiversity also from extreme habitats...
May 13, 2017: New Biotechnology
https://www.readbyqxmd.com/read/28508381/visualization-of-metallodrugs-in-single-cells-by-secondary-ion-mass-spectrometry-imaging
#5
REVIEW
Kui Wu, Feifei Jia, Wei Zheng, Qun Luo, Yao Zhao, Fuyi Wang
Secondary ion mass spectrometry, including nanoscale secondary ion mass spectrometry (NanoSIMS) and time-of-flight secondary ion mass spectrometry (ToF-SIMS), has emerged as a powerful tool for biological imaging, especially for single cell imaging. SIMS imaging can provide information on subcellular distribution of endogenous and exogenous chemicals, including metallodrugs, from membrane through to cytoplasm and nucleus without labeling, and with high spatial resolution and chemical specificity. In this mini-review, we summarize recent progress in the field of SIMS imaging, particularly in the characterization of the subcellular distribution of metallodrugs...
May 15, 2017: Journal of Biological Inorganic Chemistry: JBIC
https://www.readbyqxmd.com/read/28508122/a-trivalent-enzymatic-system-for-uricolytic-therapy-of-hprt-deficiency-and-lesch-nyhan-disease
#6
Luca Ronda, Marialaura Marchetti, Riccardo Piano, Anastasia Liuzzi, Romina Corsini, Riccardo Percudani, Stefano Bettati
PURPOSE: Because of the evolutionary loss of the uricolytic pathway, humans accumulate poorly soluble urate as the final product of purine catabolism. Restoration of uricolysis through enzyme therapy is a promising treatment for severe hyperuricemia caused by deficiency of hypoxanthine-guanine phosphoribosyltransferase (HPRT). To this end, we studied the effect of PEG conjugation on the activity and stability of the enzymatic complement required for conversion of urate into the more soluble (S)-allantoin...
May 15, 2017: Pharmaceutical Research
https://www.readbyqxmd.com/read/28504366/mechanochemical-synthesis-of-phosphazane-based-frameworks
#7
Ying Sim, Yan X Shi, Rakesh Ganguly, Yongxin Li, Felipe Garcia
Mechanochemistry is emerging as an powerful solvent-free approach to chemical synthesis, having been applied to metal oxides, pharmaceutical materials, organic compounds and to a lesser extent, coordination complex synthesis. Notably, examples of applications of mechanochemical methodologies in the synthesis of main group compounds are few and far between. Herein, we demonstrate that ball-milling enabled the solvent-free synthesis of a range of phosphazane frameworks with a broad substrate scope, yielding seven new acyclic and macrocyclic species...
May 15, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28487120/surface-anchored-counterions-on-weak-chiral-anion-exchangers-accelerate-separations-and-improve-their-compatibility-for-mass-spectrometry-hyphenation
#8
Ulrich Woiwode, Adrian Sievers-Engler, Aleksandra Zimmermann, Wolfgang Lindner, Orlando L Sánchez-Muñoz, Michael Lämmerhofer
In the present work we propose new variants of chiral stationary phases (CSP) with tert-butylcarbamoylquinine (tBuCQN) as chiral selector molecule. Four tBuCQN-CSPs with distinct bonding chemistries are compared in terms of their pH-dependent surface charge by ζ-potential determinations, by achiral and chiral liquid chromatographic tests and LC-ESI-MS hyphenation. In one embodiment tBuCQN was immobilized on 3-mercaptopropylmethylsilyl-modified silica by thiol-ene click reaction (brush type CSP with selector coverage of 0...
April 28, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28474553/metal-complex-peptide-conjugates-how-to-modulate-bioactivity-of-metal-containing-compounds-by-the-attachment-to-peptides
#9
Ines Neundorf
During the last years the interest in combining the features of metal-containing molecules with biomolecules, particularly peptides, has more and more increased. Large series of new innovative organometallic compounds, as well as potent coordination complexes have been designed and, especially in medicinal chemistry, the library of bioactive compounds was excessively expanded by the introduction of metal complexes. The research foci are divers and not limited to e.g. the development of therapeutics with anti-proliferative or antibacterial activity, or the design of novel biosensors useful for pharmaceutical applications...
May 4, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28474140/comparison-of-psma-hbed-and-psma-i-t-as-diagnostic-agents-in-prostate-carcinoma
#10
Michael McCarthy, Tiffany Langton, Divesh Kumar, Andrew Campbell
PURPOSE: Gallium(68)-labelled prostate-specific membrane antigen (PSMA) radiopharmaceuticals can be used to detect prostate cancer (PCa) cells due the their over expression of PSMA. The (68)Ga HBED-PSMA (PSMA-HBED) ligand has been most widely used and can be considered the current gold standard agent. Further PSMA ligands based on the DOTAGA and DOTA conjugates have more recently been developed. These agents (PSMA-I&T and PSMA-617) have potential theranostic capabilities as they can be conjugated with therapeutic radioisotopes...
May 4, 2017: European Journal of Nuclear Medicine and Molecular Imaging
https://www.readbyqxmd.com/read/28466691/salt-selection-matters-differential-renal-toxicity-with-mdv1634-maleate-versus-mdv1634-2hcl
#11
Mausumee Guha, Linh Nguyen, Florence Poitout-Belissent, Agathe Bedard, Kavita Raman
Salt forms of pharmaceutical compounds can have unique pharmacokinetic and toxicity properties. MDV1634 was evaluated for neurology indication and also demonstrated blood pressure (BP)-lowering effects in nonclinical studies. During the chemistry manufacturing campaign, 2 salt forms, dihydrochloride (2HCl) and maleate (MAL), which improved chemical stability and water solubility of the free base were identified. MDV1634.MAL showed better chemical attributes and was evaluated in toxicology studies for further development...
January 1, 2017: International Journal of Toxicology
https://www.readbyqxmd.com/read/28466644/development-of-halogenase-enzymes-for-use-in-synthesis
#12
Jonathan Latham, Eileen Brandenburger, Sarah A Shepherd, Binuraj R K Menon, Jason Micklefield
Nature has evolved halogenase enzymes to regioselectively halogenate a diverse range of biosynthetic precursors, with the halogens introduced often having a profound effect on the biological activity of the resulting natural products. Synthetic endeavors to create non-natural bioactive small molecules for pharmaceutical and agrochemical applications have also arrived at a similar conclusion: halogens can dramatically improve the properties of organic molecules for selective modulation of biological targets in vivo...
May 3, 2017: Chemical Reviews
https://www.readbyqxmd.com/read/28462396/photochemical-perfluoroalkylation-with-pyridine-n-oxides-mechanistic-insights-and-performance-on-a-kilogram-scale
#13
Joel W Beatty, James J Douglas, Richard Miller, Rory C McAtee, Kevin P Cole, Corey R J Stephenson
The direct trifluoromethylation of (hetero)arenes is a process of high importance to the pharmaceutical industry. Many reagents exist for this purpose and have found widespread use in discovery efforts; however, the step-intensive preparation of these reagents and their corresponding cost have resulted in minimal use of these methods in large-scale applications. For the ready transition of direct trifluoromethylation methodologies to large-scale application, the further development of processes utilizing inexpensive CF3 sources available on a metric ton scale is highly desirable...
September 8, 2016: Chem
https://www.readbyqxmd.com/read/28461231/calculation-of-a-permitted-daily-exposure-value-for-the-solvent-2-methyltetrahydrofuran
#14
Patricia Parris, J Neil Duncan, Andrew Fleetwood, William P Beierschmitt
In response to increasing concerns around the potential environmental impact of industrial chemicals, the pharmaceutical industry is seeking alternatives for traditional solvents used during the manufacturing process. Taking into consideration the principles of green chemistry, 2-methyltetrahydrofuran (2-MeTHF) is proposed as a suitable replacement for the structurally similar solvent tetrahydrofuran (THF). 2-MeTHF is derived from renewable sources and is more easily recovered thereby facilitating its reuse...
April 29, 2017: Regulatory Toxicology and Pharmacology: RTP
https://www.readbyqxmd.com/read/28455535/one-step-fabrication-of-ph-responsive-membranes-and-microcapsules-through-interfacial-h-bond-polymer-complexation
#15
Julien Dupré de Baubigny, Corentin Trégouët, Thomas Salez, Nadège Pantoustier, Patrick Perrin, Mathilde Reyssat, Cécile Monteux
Biocompatible microencapsulation is of widespread interest for the targeted delivery of active species in fields such as pharmaceuticals, cosmetics and agro-chemistry. Capsules obtained by the self-assembly of polymers at interfaces enable the combination of responsiveness to stimuli, biocompatibility and scaled up production. Here, we present a one-step method to produce in situ membranes at oil-water interfaces, based on the hydrogen bond complexation of polymers between H-bond acceptor and donor in the oil and aqueous phases, respectively...
April 28, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28451225/ru-catalyzed-sequence-for-the-synthesis-of-cyclic-amido-ethers
#16
Barry M Trost, Ehesan U Sharif, James J Cregg
Efficient synthesis of versatile building blocks for enabling medicinal chemistry research has always challenged synthetic chemists to develop innovative methods. Of particular interest are the methods that are amenable to the synthesis of chemically distinct and diverse classes of pharmaceutically relevant motifs. Herein we report a general method for the one-pot synthesis of cyclic α-amido-ethers containing different amide functionalities including lactams, tetramic acids and amino acids. For the incorporation of the nucleotide bases, a chemo and regioselective palladium-catalyzed transformation has been developed, providing rapid access to nucleoside analogs...
January 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28451148/site-selective-suzuki-miyaura-coupling-of-heteroaryl-halides-understanding-the-trends-for-pharmaceutically-important-classes
#17
Joshua Almond-Thynne, David C Blakemore, David C Pryde, Alan C Spivey
Suzuki-Miyaura cross-coupling reactions of heteroaryl polyhalides with aryl boronates are surveyed. Drawing on data from literature sources as well as bespoke searches of Pfizer's global chemistry RKB and CAS Scifinder® databases, the factors that determine the site-selectivity of these reactions are discussed with a view to rationalising the trends found.
January 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28445767/the-visualized-macrocycles-chemistry-and-application-of-fluorophore-tagged-cyclodextrins
#18
Gábor Benkovics, Milo Malanga, Éva Fenyvesi
Cyclodextrins are macrocyclic molecules able to form host-guest complexes due to their hydrophobic cavity. Because of their carbohydrate nature they do not absorb light in the UV-vis region (200-800nm), but they can be converted into spectroscopically active compounds via modification with a chromophore unit. Among the chromophores, the group of fluorophores can provide high sensitivity in analytical applications (chemosensing) and low detection limit in optical imaging methods (fluorescent microscopy). Fluorophore-tagged cyclodextrins therefore combine interesting spectroscopic properties with promising supramolecular features which make these conjugates widely applicable in various pharmaceutical fields...
April 23, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28443923/use-of-alcl3-in-friedel-crafts-arylation-type-reactions-and-beyond-an-overview-on-the-development-of-unique-methodologies-leading-to-n-heteroarenes
#19
REVIEW
Rajnikanth Sunke, Suresh Babu Nallapati, Jetta Sandeep Kumar, K Shiva Kumar, Manojit Pal
As a privileged class of heterocyclic compounds N-heteroarenes have found enormous applications in many areas including medicinal/pharmaceutical chemistry and drug discovery. Consequently, a wide variety of methods have been reported for their synthesis. While not free from their own limitations the AlCl3 mediated methods appeared to have some particular advantages in preparing a number of useful N-heteroarenes. Besides the famous Friedel-Crafts (FC) alkylation/acylation reactions one such example is AlCl3-induced heteroarylation of arenes and heteroarenes (FC arylation type reactions) that can be used to prepare a certain class of N-heteroarenes in an operationally simple, efficient and cost effective manner...
May 16, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28442707/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 23, 2016: Scientific Reports
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