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https://www.readbyqxmd.com/read/29227923/in-vitro-leishmanicidal-and-trypanocidal-evaluation-and-magnetic-properties-of-7-amino-1-2-4-triazolo-1-5-a-pyrimidine-cu-ii-complexes
#1
J M Méndez-Arriaga, I Oyarzabal, G Escolano, A Rodríguez-Diéguez, M Sánchez-Moreno, J M Salas
Two triazolopyrimidine complexes have been obtained from reaction between 7-amino-1,2,4-triazolo[1,5-a]pyrimidine (7atp) and Cu (II) salts. Crystal structures of [Cu2(μ-7atp)4Cl2]Cl2·4H2O (1) and [Cu2(μ-7atp)4(H2O)2](NO3)4·H2O (2) have been studied by X-ray diffraction methods and characterized by spectroscopic and thermal analysis. Magnetic studies of these dinuclear complexes have revealed the existence of moderate antiferromagnetic interactions between the copper ions, with J values of -91.2 and -96...
December 2, 2017: Journal of Inorganic Biochemistry
https://www.readbyqxmd.com/read/29227917/design-synthesis-molecular-docking-of-new-lipophilic-acetamide-derivatives-affording-potential-anticancer-and-antimicrobial-agents
#2
Hany E A Ahmed, Saleh K Ihmaid, Abdelsattar M Omar, Ahmed M Shehata, Heba S Rateb, Mohammed F Zayed, Sahar Ahmed, Mahmoud M Elaasser
Fifteen new substituted N-2-(2-oxo-3-phenylquinoxalin-1(2H)-yl) acetamides 5a-f, 6a-f, and 8a-c were synthesized by reacting ethyl 2-(2-oxo-3-phenylquinoxalin-1(2H)-yl)acetate with various primary amines including benzylamines, sulfonamides, and amino acids. The in vitro antimicrobial screening of the target compounds was screened to assess their antibacterial and antifungal activity. As a result, seven compounds namely; 5a, 5c, 5d, 6a, 6c, 8b and 8c showed a promising broad spectrum antibacterial activity against both Gram-positive and Gram-negative strains...
December 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29227631/helium-ion-microscopy-for-imaging-and-quantifying-porosity-at-the-nanoscale
#3
Matthew J Burch, Anton V Ievlev, Kyle Mahady, Holland Hysmith, Philip D Rack, Alex Belianinov, Olga S Ovchinnikova
Nano-porous materials are key components in a vast number of applications from energy, to drug delivery and to agriculture. However, the number of ways to analytically quantify the salient features in these materials, e.g. surface structure, pore shape, and size, remain limited. The most common approach is gas absorption, where volumetric gas absorption and desorption are measured. This technique has some fundamental drawbacks such as low sample throughput and a lack of direct surface visualization. In this work, we demonstrate Helium Ion Microscopy (HIM) as a tool for imaging and quantification of pores in industrially relevant SiO2 catalyst supports...
December 11, 2017: Analytical Chemistry
https://www.readbyqxmd.com/read/29227540/human-t-lymphotropic-virus-1-htlv-1-pathogenesis-a-systems-virology-study
#4
Sayed-Hamidreza Mozhgani, Mohadeseh Zarei Ghobadi, Majid Teymoori-Rad, Talat Mokhtari Azad, Mehdi Mirzaie, Mohsen Sheikhi, Seyed Mohammad Jazayeri, Ramin Shabahrami, Hedayatollah Ghourchian, Mohieddin Jafari, Seyed Abdolrahim Rezaee, Mehdi Norouzi
The main mechanisms of interaction between Human T-lymphotropic virus type 1 (HTLV-1) and its hosts in manifestation of related diseases including HTLV-1 associated myelopathy/tropical spastic paraparesis (HAM/TSP) and Adult T-cell leukemia/lymphoma (ATLL) are yet to be determined. It is pivotal to find out the changes in the genes expression toward an asymptomatic or symptomatic states. To this end, the systems virology analysis was performed. Firstly, the differentially expressed genes (DEGs) were taken pairwise among the four sample sets of Normal, Asymptomatic Carriers (ACs), ATLL, and HAM/TSP...
December 11, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/29227526/bioactive-peptides-derived-from-seaweed-protein-and-their-health-benefits-antihypertensive-antioxidant-and-antidiabetic-properties
#5
REVIEW
Habtamu Admassu, Mohammed Abdalbasit A Gasmalla, Ruijin Yang, Wei Zhao
Cardiovascular diseases and diabetes are the biggest causes of death globally. Therefore, prevention of these diseases is a focus of pharmaceuticals and functional food manufacturers. This review summarizes recent research trends and scientific knowledge in seaweed protein-derived peptides with particular emphasis on production, isolation and potential health impacts in prevention of hypertension, diabetes and oxidative stress. The current status and future prospects of bioactive peptides are also discussed...
December 11, 2017: Journal of Food Science
https://www.readbyqxmd.com/read/29227473/structure-inspired-design-of-%C3%AE-arrestin-biased-ligands-for-aminergic-gpcrs
#6
John D McCorvy, Kyle V Butler, Brendan Kelly, Katie Rechsteiner, Joel Karpiak, Robin M Betz, Bethany L Kormos, Brian K Shoichet, Ron O Dror, Jian Jin, Bryan L Roth
Development of biased ligands targeting G protein-coupled receptors (GPCRs) is a promising approach for current drug discovery. Although structure-based drug design of biased agonists remains challenging even with an abundance of GPCR crystal structures, we present an approach for translating GPCR structural data into β-arrestin-biased ligands for aminergic GPCRs. We identified specific amino acid-ligand contacts at transmembrane helix 5 (TM5) and extracellular loop 2 (EL2) responsible for Gi/o and β-arrestin signaling, respectively, and targeted those residues to develop biased ligands...
December 11, 2017: Nature Chemical Biology
https://www.readbyqxmd.com/read/29227117/an-autopsy-case-of-death-by-combined-use-of-benzodiazepines-and-diphenidine
#7
Hiroshi Kinoshita, Naoko Tanaka, Ayaka Takakura, Hiroko Abe, Mitsuru Kumihashi, Takayuki Shibayama, Mostofa Jamal, Asuka Ito, Kunihiko Tsutsui, Shoji Kimura, Hirotaro Iwase, Kiyoshi Ameno
We present an autopsy case involving benzodiazepines and diphenidine. Quantitative toxicological analysis showed concentrations of 7-aminoflunitrazepam (a flunitrazepam metabolite), 7-aminonimetazepam (a nimetazepam metabolite), chlorpheniramine and diphenidine in femoral blood of 0.086 µg/ml, 0.027 µg/ml, 0.066 µg/ml, and 0.073 µg/ml, respectively. Death was attributed to combined toxicity due to the influence of multiple drug interactions.
2017: Soudní Lékarství
https://www.readbyqxmd.com/read/29227101/the-magic-of-crystal-structure-based-inhibitor-optimization-development-of-a-butyrylcholinesterase-inhibitor-with-picomolar-affinity-and-in-vivo-activity
#8
Urban Košak, Boris Brus, Damijan Knez, Simon Žakelj, Jurij Trontelj, Anja Pišlar, Roman Šink, Marko Jukič, Marko Živin, Adrian Podkowa, Florian Nachon, Xavier Brazzolotto, Jure Stojan, Janko Kos, Nicolas Coquelle, Kinga Salat, Jacques-Philippe Colletier, Stanislav Gobec
The enzymatic activity of butyrylcholinesterase (BChE) in the brain increases with the progression of Alzheimer's disease, thus classifying BChE as a promising drug target in advanced Alzheimer's disease. We used structure-based drug-discovery approaches to develop potent, selective and reversible human BChE inhibitors. The most potent, compound 3, had a picomolar inhibition constant versus BChE due to strong cation-π interactions, as revealed by the solved crystal structure of its complex with human BChE...
December 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29226922/a-polymyxin-b-silver-nanoparticle-colloidal-system-and-the-application-of-lipopolysaccharide-analysis
#9
Tao Liu, Liqian Gao, Jing Zhao, Ya Cao, Yuguo Tang, Peng Miao
Polymyxin B (PMB) is a small cyclic polycationic lipopeptide, which can be used as an antibiotic drug against Gram-negative bacteria. In this work, the interaction between citrate capped silver nanoparticles (AgNPs) and PMB is studied. Experimental results show that the association constant is extremely high and the binding event leads to a significant variation in the localized surface plasmon resonance (LSPR) of AgNPs. Moreover, the PMB-AgNP colloidal system can be further exploited as a sensitive analytical platform...
December 11, 2017: Analyst
https://www.readbyqxmd.com/read/29226685/size-effect-on-lipid-nanocapsules-mediated-glp-1-secretion-from-enteroendocrine-l-cells
#10
Yining Xu, Dario Carradori, Mireille Alhouayek, Giulio G Muccioli, Patrice D Cani, Veronique Preat, Ana Beloqui
L cells are enteroendocrine cells located throughout the gastrointestinal tract that secrete physiologically important peptides. The most characterized peptides secreted by L cells are the peptide YY (PYY) and the glucagon-like peptide (GLP) -1 and -2. These peptides are released rapidly into the circulation after oral nutrient ingestion. Recently, lipid-based nanoparticles (NP) have been described as triggers for GLP-1 secretion by L cells. NP physicochemical properties play a key role in the NP-cell interaction, and drive NP cell internalization...
December 11, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29226628/modeling-of-prolactin-response-following-dopamine-d2-receptor-antagonists-in-rats-can-it-be-translated-to-clinical-dosing
#11
Amit Taneja, An Vermeulen, Dymphy R H Huntjens, Meindert Danhof, Elizabeth C M De Lange, Johannes H Proost
Prolactin release is a side effect of antipsychotic therapy with dopamine antagonists, observed in rats as well as humans. We examined whether two semimechanistic models could describe prolactin response in rats and subsequently be translated to predict pituitary dopamine D2 receptor occupancy and plasma prolactin concentrations in humans following administration of paliperidone or remoxipride. Data on male Wistar rats receiving single or multiple doses of risperidone, paliperidone, or remoxipride was described by two semimechanistic models, the precursor pool model and the agonist-antagonist interaction model...
December 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29226626/randomized-clinical-study-of-safety-pharmacokinetics-and-pharmacodynamics-of-ripk1-inhibitor-gsk2982772-in-healthy-volunteers
#12
Kathleen Weisel, Nicola E Scott, Debra J Tompson, Bartholomew J Votta, Sujith Madhavan, Kat Povey, Allen Wolstenholme, Monica Simeoni, Todd Rudo, Lauren Richards-Peterson, Tarjinder Sahota, J Gene Wang, John Lich, Joshua Finger, Adeline Verticelli, Michael Reilly, Peter J Gough, Philip A Harris, John Bertin, Mei-Lun Wang
GSK2982772 is a highly selective inhibitor of receptor-interacting protein kinase 1 (RIPK1) being developed to treat chronic inflammatory diseases. This first-in-human study evaluated safety, tolerability, pharmacokinetics (PK), and exploratory pharmacodynamics (PD) of GSK2982772 administered orally to healthy male volunteers. This was a Phase I, randomized, placebo-controlled, double-blind study. In Part A, subjects received single ascending doses of GSK2982772 (0.1-120 mg) or placebo in a crossover design during each of 4 treatment periods...
December 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/29226313/model-based-assessments-of-cyp-mediated-drug-drug-interaction-risk-of-alectinib-physiologically-based-pharmacokinetic-modeling-supported-clinical-development
#13
Yumi Cleary, Michael Gertz, Peter N Morcos, Li Yu, Kuresh Youdim, Alex Phipps, Stephen Fowler, Neil Parrott
Alectinib is a selective anaplastic lymphoma kinase (ALK) inhibitor approved for the treatment of ALK-positive non-small cell lung cancer. Alectinib and its major active metabolite M4 exhibited drug-drug interaction (DDI) potential through cytochrome P450 (CYP) enzymes CYP3A4 and CYP2C8 in vitro. Clinical relevance of the DDI risk was investigated as part of a rapid development program to fulfil the breakthrough therapy designation. Therefore, a strategy with a combination of physiologically based pharmacokinetic (PBPK) modeling and limited clinical trials focused on generating informative data for modeling was taken to ensure extrapolation ability of DDI risk...
December 11, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29226142/computational-exploration-for-lead-compounds-that-can-reverse-the-nuclear-morphology-in-progeria
#14
Shailima Rampogu, Ayoung Baek, Minky Son, Amir Zeb, Chanin Park, Raj Kumar, Gihwan Lee, Donghwan Kim, Yeonuk Choi, Yeongrae Cho, Yohan Park, Seok Ju Park, Keun Woo Lee
Progeria is a rare genetic disorder characterized by premature aging that eventually leads to death and is noticed globally. Despite alarming conditions, this disease lacks effective medications; however, the farnesyltransferase inhibitors (FTIs) are a hope in the dark. Therefore, the objective of the present article is to identify new compounds from the databases employing pharmacophore based virtual screening. Utilizing nine training set compounds along with lonafarnib, a common feature pharmacophore was constructed consisting of four features...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29226062/interactions-of-protonated-guanidine-and-guanidine-derivatives-with-multiply-deprotonated-rna-probed-by-electrospray-ionization-and-collisionally-activated-dissociation
#15
Jovana Vušurović, Eva-Maria Schneeberger, Kathrin Breuker
Interactions of ribonucleic acid (RNA) with guanidine and guanidine derivatives are important features in RNA-protein and RNA-drug binding. Here we have investigated noncovalently bound complexes of an 8-nucleotide RNA and six different ligands, all of which have a guanidinium moiety, by using electrospray ionization (ESI) and collisionally activated dissociation (CAD) mass spectrometry (MS). The order of complex stability correlated almost linearly with the number of ligand atoms that can potentially be involved in hydrogen-bond or salt-bridge interactions with the RNA, but not with the proton affinity of the ligands...
December 2017: ChemistryOpen
https://www.readbyqxmd.com/read/29225544/novel-targets-for-developing-antiseizure-and-potentially-antiepileptogenic-drugs
#16
Dipan C Patel, Karen S Wilcox, Cameron S Metcalf
Epilepsy is a chronic neurological disorder caused by abnormal changes in the functions of neuronal circuits and manifested by seizures. It affects patients of all age, substantially worsens the quality of life for the patients as well as their families, and imposes a huge economic burden on the healthcare system. Historically, efforts for discovering and developing antiseizure therapies have been focused on modulating the functions of receptors, transporters, and enzymes expressed by neurons. These drug development efforts have paid off, as we have over 25 antiseizure drugs available in the clinic...
September 2017: Epilepsy Currents
https://www.readbyqxmd.com/read/29225511/the-crystalline-sponge-method-a-solvent-based-strategy-to-facilitate-noncovalent-ordered-trapping-of-solid-and-liquid-organic-compounds
#17
Timothy R Ramadhar, Shao-Liang Zheng, Yu-Sheng Chen, Jon Clardy
A strategy that leverages solvent effects to noncovalently trap solid and unstable liquid organic compounds within a crystalline sponge ({[(ZnI2)3(tris(4-pyridyl)-1,3,5-triazine)2]·x(CHCl3)}n) in a simple, mild, and efficient fashion for target molecule structure determination via X-ray diffraction is disclosed. Host-guest structures were obtained using third-generation synchrotron radiation, and new beamline hardware allowed rapid data collection in ~5-24 minutes. This is 40-90% faster than previously reported crystalline sponge synchrotron datasets collected by us, and approximately a 150-720-fold decrease in time versus using a typical in-house diffractometer, effectively enabling the potential for high-throughput analysis...
August 21, 2017: CrystEngComm
https://www.readbyqxmd.com/read/29225461/risperidone-mucoadhesive-buccal-tablets-formulation-design-optimization-and-evaluation
#18
Burak Çelik
The aim of this study was to design and optimize risperidone (RIS) mucoadhesive buccal tablets for systemic delivery as an alternative route. Direct compression method was used for the preparation of buccal tablets, and screening studies were conducted with different polymers to determine their effects on tablet characteristics. Carbopol® (CP) and sodium alginate (SA) were selected as two polymer types for further optimization studies by applying response surface methodology. Tablet hardness (TH), ex vivo residence time (RT), and peak detachment force (DF) from buccal mucosa were selected as three important responses...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/29225432/molecular-docking-based-screening-of-a-simulated-hif-1-protein-model-for-potential-inhibitors
#19
Mundla Sri Latha, Madhu Sudhana Saddala
Hypoxia inducible factor-1(HIF-1) is a bHLH-family transcription factor that control genes involved in glucolysis, angiogenesis, migration, as well as invasion factors that are important for tumor progression and metastasis. HIF-1, a hetero dimer of HIF-1α and HIF-1β, binds to the hypoxia responsive genes, such as vascular endothelial growth factor (VEGF). It is one the molecular target for angiogenesis. A series of Chalcone - like compounds described that preferentially inhibit HIF-1 dimer, which can interact with amino acids within the active site of the protein...
2017: Bioinformation
https://www.readbyqxmd.com/read/29225192/effects-of-the-new-psychoactive-substances-diclofensine-diphenidine-and-methoxphenidine-on-monoaminergic-systems
#20
Dino Luethi, Marius C Hoener, Matthias E Liechti
Diclofensine, diphenidine, and methoxphenidine are new psychoactive substances (NPSs) that recently appeared on the illicit drug market. Pharmacological profiling of such newly emerged drugs is crucial for a better understanding of their psychotropic effects and toxicity. We therefore investigated the potential of these NPSs to inhibit the norepinephrine, dopamine, and serotonin transporters in human embryonic kidney cells stably transfected with the respective transporters. In addition, we determined monoamine transporter and receptor affinities for the substances...
December 7, 2017: European Journal of Pharmacology
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