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https://www.readbyqxmd.com/read/29241294/early-stage-formulation-considerations
#1
Robert W Lee, Mark Mitchnick
When a drug candidate-i.e., a new chemical entity (NCE) or new molecular entity (NME)-is discovered, there is a requirement to identify a vehicle for in vitro and/or in vivo evaluation to assess the activity and/or toxicity of the compound (here we refer to the biologically active compound as the active pharmaceutical ingredient: API). Ideally, this vehicle will not impart any biological activity or any toxicity that would mask or confound the effects of the API. At this early stage in development, and given the high attrition rates of drug candidates in discovery, it does not make sense to fully characterize the API-speed and cost are generally the driving factors...
December 14, 2017: Current Protocols in Chemical Biology
https://www.readbyqxmd.com/read/29241196/calycosin-inhibits-the-migration-and-invasion-of-human-breast-cancer-cells-by-down-regulation-of-foxp3-expression
#2
Shuangxi Li, Yafei Wang, Chan Feng, Guoli Wu, Yu Ye, Jing Tian
BACKGROUND/AIMS: Calycosin, a phytoestrogenic compound, has recently emerged as a promising antitumor drug. It has been shown that calycosin suppresses growth and induces apoptosis of breast cancer cells. However, the effect of calycosin on migration and invasion of breast cancer cells and the underlying molecular mechanisms have not been elucidated. METHODS: Human breast cancer cells MCF-7 and T47D were treated with, or without, different doses (0, 6.25, 12.5, 25, 50, 100 or 150 μM) of calycosin, and the viability of different groups was determined by MTT assay...
December 6, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/29241144/the-diverse-reasons-for-using-novel-psychoactive-substances-a-qualitative-study-of-the-users-own-perspectives
#3
Christophe Soussan, Martin Andersson, Anette Kjellgren
BACKGROUND: The increasing number of legally ambiguous and precarious Novel Psychoactive Substances (NPS) constitutes a challenge for policy makers and public health. Scientific and more in-depth knowledge about the motivations for using NPS is scarce and often consist of predetermined, non-systematic, or poorly described reasons deduced from top-down approaches. Therefore, the aim of the present study was to explore and characterize the users' self-reported reasons for NPS use inductively and more comprehensively...
December 11, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29241093/quantitative-analysis-of-drugs-in-hair-by-uhplc-high-resolution-mass-spectrometry
#4
Robert Kronstrand, Malin Forsman, Markus Roman
Liquid chromatographic methods coupled to high resolution mass spectrometry are increasingly used to identify compounds in various matrices including hair but there are few recommendations regarding the parameters and their criteria to identify a compound. In this study we present a method for the identification and quantification of a range of drugs and discuss the parameters used to identify a compound with high resolution mass spectrometry. Drugs were extracted from hair by incubation in a buffer:solvent mixture at 37°C during 18h...
December 8, 2017: Forensic Science International
https://www.readbyqxmd.com/read/29240870/practitioners-take-huge-risks-dealing-with-rogue-drug-compounders
#5
Sheldon Bradshaw
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December 1, 2017: Journal of Drugs in Dermatology: JDD
https://www.readbyqxmd.com/read/29240773/polypyridylruthenium-ii-complexes-exert-anti-schistosome-activity-and-inhibit-parasite-acetylcholinesterases
#6
Madhu K Sundaraneedi, Bemnet Tedla, Ramon M Eichenberger, Luke Becker, Darren Pickering, Michael J Smout, Siji Rajan, Phurpa Wangchuk, F Richard Keene, Alex Loukas, J Grant Collins, Mark S Pearson
BACKGROUND: Schistosomiasis affects over 200 million people and there are concerns whether the current chemotherapeutic control strategy (periodic mass drug administration with praziquantel (PZQ)-the only licenced anti-schistosome compound) is sustainable, necessitating the development of new drugs. METHODOLOGY/PRINCIPAL FINDINGS: We investigated the anti-schistosome efficacy of polypyridylruthenium(II) complexes and showed they were active against all intra-mammalian stages of S...
December 14, 2017: PLoS Neglected Tropical Diseases
https://www.readbyqxmd.com/read/29240701/25th-conference-of-gp2a
#7
Michael D Threadgill, Susan E Matthews, Francesca Giuntini
The 25th Conference of GP2A was held on 31 August and 1 September 2017 in Liverpool, UK, with the aim of exchange of ideas and experience, particularly amongst young medicinal chemists. Topics included bioactive compounds from plants and lichens, and design and development of drugs. Abstracts of invited lectures, proffered oral presentations, flash presentations and posters presented during the meeting are collected in this report.
December 14, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/29240615/enhancement-and-suppression-of-ionisation-in-drug-analysis-using-hplc-ms-ms-in-support-of-therapeutic-drug-monitoring-a-review-of-current-knowledge-of-its-minimisation-and-assessment
#8
Rani George, Alison Haywood, Sohil Khan, Mirjana Radovanovic, Joshua Simmonds, Ross Norris
High-performance liquid chromatography coupled with tandem mass spectrometry (HPLC-MS/MS) is commonly used for quantitation of analytes in biological matrices, due to the selectivity, sensitivity, and high throughput offered by this technique. However, the presence of both suppression and enhancement of ionization (SEI) by matrix components is an increasingly recognized impediment to accurate results. The existence of SEI indicates that ionization efficiency is a result of the chemical environment seen by both the analyte and internal standard during ion formation...
December 11, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29240409/from-experiments-to-a-fast-easy-to-use-computational-methodology-to-predict-human-aldehyde-oxidase-selectivity-and-metabolic-reactions
#9
Gabriele Cruciani, Nicolò Milani, Paolo Benedetti, Susan Lepri, Lucia Cesarini, Massimo Baroni, Francesca Spyrakis, Sara Tortorella, Edoardo Mosconi, Laura Goracci
Aldehyde oxidase (AOX) is a molibdo-flavoenzyme that raised great interest in recent years, since its contribution in xenobiotics metabolism has not always been identified before clinical trials, with consequent negative effects on the fate of new potential drugs. The fundamental role of AOX in metabolizing xenobiotics is also due to the attempt of medicinal chemists to stabilize candidates toward cytochrome P450 activity, which increases the risk for new compounds to be susceptible to AOX nucleophile attack...
December 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29240402/structural-basis-of-aldh1a2-inhibition-by-irreversible-and-reversible-small-molecule-inhibitors
#10
Yan Chen, Jin-Yi Zhu, Kwon Ho Hong, David C Mikles, Gunda I Georg, Alex S Goldstein, John K Amory, Ernst Schönbrunn
The ALDH1A subfamily of aldehyde dehydrogenase enzymes are crucial in regulating retinoic acid (RA) signaling and have received attention as potential drug targets. ALDH1A2 is the primary RA-synthesizing enzyme in mammalian spermatogenesis and is therefore considered a viable drug target for male contraceptive development. However, only a small number of ALDH1A2 inhibitors have been reported, and information on the structure of ALDH1A2 was limited to the NAD-liganded enzyme void of substrate or inhibitors. Herein, we describe the mechanism of action of structurally unrelated reversible and irreversible inhibitors of human ALDH1A2 using direct binding studies and X-ray crystallography...
December 14, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/29240291/novel-4-amino-1-2-3-triazole-inhibitors-of-indoleamine-2-3-dioxygenase-form-a-long-lived-complex-with-the-enzyme-and-display-exquisite-cellular-potency
#11
Julie Alexandre, Michael Swan, Mike Latchem, Dean Boyall, John Pollard, Stuart Hughes, James Westcott
Indoleamine-2,3 dioxygenase (IDO) has emerged as a central regulator of immune responses in both normal and disease biology. Due to its established role in promoting tumour immune escape, IDO has become an attractive target for cancer treatment. We have identified a novel series of highly cell potent IDO inhibitors based on a 4-amino-1,2,3-triazole core. Comprehensive kinetic, biochemical and structural studies demonstrate that compounds from this series have a non-competitive kinetic mechanism-of-action with respect to the tryptophan substrate...
December 14, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/29239940/prolonged-duration-local-anesthesia-using-liposomal-bupivacaine-combined-with-liposomal-dexamethasone-and-dexmedetomidine
#12
Alina Y Rwei, Robert T Sherburne, David Zurakowski, Bruce Wang, Daniel S Kohane
BACKGROUND: The relatively short duration of effect of local anesthetics has been addressed by encapsulation in drug delivery systems. Codelivery with a single compound that produces an adjuvant effect on nerve block but without intrinsic local anesthetic properties can further prolong the nerve block effect. Here, we investigated whether codelivery of more than 1 encapsulated adjuvant compound can further enhance nerve blockade. METHODS: Liposomes loaded with bupivacaine (Bup), dexamethasone phosphate (DexP), or dexmedetomidine (DMED) were synthesized and its in vitro drug release profiles were determined...
December 11, 2017: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29239784/new-perspectives-for-natural-triterpene-glycosides-as-potential-adjuvants
#13
Marie-Aleth Lacaille-Dubois, Hildebert Wagner
BACKGROUND: Triterpene glycosides are a vast group of secondary metabolites widely distributed in plants including a high number of biologically active compounds. The pharmacological potential is evaluated by using many bioassays particularly in the field of cancerology, immunology, and microbiology. The adjuvant concept is well known for these molecules in vaccines, but there is little preclinical evidence to support this concept in the management of cancer, infections and inflammation...
November 7, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/29239714/fusion-proteins-towards-fungi-and-bacteria-in-plant-protection
#14
Ana Margarida Pinheiro, Alexandra Carreira, Ricardo B Ferreira, Sara Monteiro
In agriculture, although fungi are considered the foremost problem, infections by bacteria also cause significant economical losses. The presence of different diseases in crops often leads to a misuse of the proper therapeutic, or the combination of different diseases forces the use of more than one pesticide. This work concerns the development of a 'super-Blad': a chimeric protein consisting of Blad polypeptide, the active ingredient of a biological fungicide already on the market, and two selected peptides, SP10-5 and Sub5, proven to possess biological potential as antibacterial agents...
December 14, 2017: Microbiology
https://www.readbyqxmd.com/read/29239018/design-synthesis-and-biological-evaluation-of-1-ethyl-3-thiazol-2-yl-urea-derivatives-as-escherichia-coli-dna-gyrase-inhibitors
#15
Tihomir Tomašič, Michaela Barančoková, Nace Zidar, Janez Ilaš, Päivi Tammela, Danijel Kikelj
Discovery of novel DNA gyrase B inhibitors remains an attractive field in the search for new antibacterial drugs to overcome the known bacterial resistance mechanisms. In the present study, we designed and synthesized novel ethylurea derivatives of 4,5,6,7-tetrahydrobenzo[1,2-d]thiazole-2,6-diamine, 2-(2-aminothiazol-4-yl)acetic acid, and benzo[1,2-d]thiazole-2,6-diamine and evaluated their Escherichia coli DNA gyrase inhibition. The most potent DNA gyrase inhibitors in the prepared library of compounds were benzo[1,2-d]thiazoles 32-34, 36, and 37 with IC50 values in the low micromolar range...
December 14, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29238994/intestinal-p-glycoprotein-inhibitors-benzoxanthone-analogues
#16
Song Wha Chae, Jaeok Lee, Jung Hyun Park, Youngjoo Kwon, Younghwa Na, Hwa Jeong Lee
OBJECTIVES: The inhibitors of P-glycoprotein (P-gp) which limits an access of exogenous compounds in the luminal membrane of the intestine have been studied to enhance the intestinal P-gp-mediated absorption of anticancer drugs. METHODS: Inhibition of the efflux pump by synthesized benzoxanthone derivatives was investigated in vitro and in vivo. MCF-7/ADR cell line was used for cytotoxicity assay and [3 H]-daunomycin (DNM) accumulation/efflux study. Eight benzoxanthone analogues were tested for their effects on DNM cytotoxicity...
December 13, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29238904/anti-inflammatory-activity-of-anti-hyperlipidemic-drug-fenofibrate-and-its-phase-i-metabolite-fenofibric-acid-in-silico-in-vitro-and-in-vivo-studies
#17
G Shyam Prasad, P Govardhan, G Deepika, V Vakdevi, R B Sashidhar
Fenofibrate, an anti-hyperlipidemic drug and its phase-I biotransformed metabolite fenofibric acid, was studied for COX-1 (PDB ID: 3N8Y) and COX-2 (PDB ID: 1PXX) inhibition potentials in silico and in vitro for their effects on human recombinant COX-2 enzyme isolated from a Baculovirus expression system in sf21 cells (EC 1.14.99.1) using a conventional spectrophotometric assay. Furthermore, the compounds were also screened for their anti-inflammatory potentials in vivo using carrageenan-induced paw oedema method in Wistar rats...
December 13, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/29238888/synthesis-and-evaluation-of-bile-acid-amides-of-formula-see-text-cyanostilbenes-as-anticancer-agents
#18
Devesh S Agarwal, Rajnish Prakash Singh, K Lohitesh, Prabhat N Jha, Rajdeep Chowdhury, Rajeev Sakhuja
A series of amino-substituted [Formula: see text]-cyanostilbene derivatives and their bile acid (cholic and deoxycholic acid) amides were designed and synthesized. A comparative study on the anticancer and antibacterial activity evaluation on the synthesized analogs was carried against the human osteosarcoma (HOS) cancer cell line, and two gram -ve (E. coli and S. typhi) and two gram [Formula: see text]ve (B. subtilis and S. aureus) bacterial strains. All the cholic acid [Formula: see text]-cyanostilbene amides showed an [Formula: see text] in the range 2-13 [Formula: see text] against human osteosarcoma cells (HOS) with the most active analog (6g) possessing an [Formula: see text] of [Formula: see text]...
December 13, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/29238715/chemopreventive-potential-of-2-3-5-4-tetrahydroxystilbene-2-o-%C3%AE-d-glucoside-on-the-formation-of-aberrant-crypt-foci-in-azoxymethane-induced-colorectal-cancer-in-rats
#19
Chien-Liang Lin, Jiiang-Huei Jeng, Chih-Chung Wu, Shu-Ling Hsieh, Guan-Cheng Huang, Wan Leung, Chining-Ting Lee, Chung-Yi Chen, Chien-Hsing Lee
2,3,5,4'-Tetrahydroxystilbene-2-O-β-D-glucoside (THSG) has been shown to have antioxidative and anti-inflammatory effects. Oxidative and inflammatory reactions are related to the development of colorectal carcinoma (CRC). In the present study, we characterized the preventive activities of THSG on colon carcinogenesis using the azoxymethane- (AOM-) mediated rat colon carcinogenesis model. F344 male rats were randomly divided into 5 groups (untreated and AOM model rats treated with or without THSG at 30, 150, or 250 mg/kg) after which the numbers of aberrant crypt foci (ACF) were assessed in the colon tissues of all rats...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29238708/longitudinal-real-world-outcomes-of-pirfenidone-in-idiopathic-pulmonary-fibrosis-in-greece
#20
Argyrios Tzouvelekis, Theodoros Karampitsakos, Paschalis Ntolios, Vasilios Tzilas, Evangelos Bouros, Evangelos Markozannes, Ioanna Malliou, Aris Anagnostopoulos, Andreas Granitsas, Paschalis Steiropoulos, Katerina Dimakou, Serafeim Chrysikos, Nikolaos Koulouris, Demosthenes Bouros
Background: Pirfenidone is an antifibrotic compound able to slow down disease progression in patients with idiopathic pulmonary fibrosis (IPF). Objective: To investigate the safety and efficacy of pirfenidone in patients with IPF in a real-life setting. Methods: This was a multicenter, retrospective, real-life, observational study for patients with IPF receiving pirfenidone. Results: We identified 92 patients with IPF receiving pirfenidone...
2017: Frontiers in Medicine
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