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https://www.readbyqxmd.com/read/27922542/generalization-of-serotonin-and-dopamine-ligands-to-the-discriminative-stimulus-effects-of-different-doses-of-%C3%A2-3-4-methylenedioxymethamphetamine
#1
Jeremy I Webster, David N Harper, Susan Schenk
Studies that have attributed the discriminative stimulus effects of ±3,4-methylenedioxymethamphetamine (MDMA) to serotonergic mechanisms typically use a relatively low training dose of 1.5 mg/kg. The role of serotonin in the discriminative stimulus effects of higher doses of MDMA is, however, unknown. Separate groups of rats were trained to discriminate MDMA (1.5 or 3.0 mg/kg) from saline using a two-lever, food-reinforced drug-discrimination procedure. Generalization tests were carried out with a range of serotonin and dopamine ligands...
December 2, 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/27921382/core-shell-silk-hydrogels-with-spatially-tuned-conformations-as-drug-delivery-system
#2
Le-Ping Yan, Joaquim M Oliveira, Ana L Oliveira, Rui L Reis
Hydrogels of spatially controlled physicochemical properties are appealing platforms for tissue engineering and drug delivery. In this study, core-shell silk fibroin (SF) hydrogels of spatially controlled conformation were developed. The core-shell structure in the hydrogels was formed by means of soaking the preformed (enzymatically crosslinked) random coil SF hydrogels in methanol. When increasing the methanol treatment time from 1 to 10 min, the thickness of the shell layer can be tuned from about 200 to about 850 μm as measured in wet status...
December 5, 2016: Journal of Tissue Engineering and Regenerative Medicine
https://www.readbyqxmd.com/read/27919897/genetic-evidence-for-cytochrome-b-qi-site-inhibition-by-4-1h-quinolone-3-diarylethers-and-antimycin-in-toxoplasma-gondii
#3
P Holland Alday, Igor Bruzual, Aaron Nilsen, Sovitj Pou, Rolf Winter, Choukri Ben Mamoun, Michael K Riscoe, J Stone Doggett
Toxoplasma gondii is an apicomplexan parasite that causes fatal and debilitating brain and eye disease. Endochin-like-quinolones (ELQs) are preclinical compounds that are efficacious against apicomplexan-caused diseases including toxoplasmosis, malaria and babesiosis. Of the ELQs, ELQ-316 has demonstrated the greatest efficacy against acute and chronic experimental toxoplasmosis. Although genetic analyses in other organisms have highlighted the importance of the cytochrome bc1 complex Qi site for ELQ sensitivity, the mechanism of action of ELQs against T...
December 5, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27919613/cellular-uptake-of-glucoheptoamidated-poly-amidoamine-pamam-g3-dendrimer-with-amide-conjugated-biotin-a-potential-carrier-of-anticancer-drugs
#4
Łukasz Uram, Magdalena Szuster, Aleksandra Filipowicz, Magdalena Zaręba, Elżbieta Wałajtys-Rode, Stanisław Wołowiec
In search for soluble derivatives of PAMAM dendrimers as potential carriers for hydrophobic drugs, the conjugates of PAMAM G3 with biotin, further converted into glycodendrimer with d-glucoheptono-1,4-lactone, were prepared. Polyamidoamine dendrimer (PAMAM) of third generation, G3 was functionalized with four biotin equivalents covalently attached to terminal amine nitrogens via amide bond G3(4B). The remaining 28 amine groups were blocked by glucoheptoamide substituents (gh) to give G3(4B28gh) or with one fluorescein equivalent (attached by reaction of G3(4B) with fluorescein isothiocyanate, FITC) via thiourea bond as FITC followed by exhaustive glucoheptoamidation to get G3(4B27gh1F)...
November 25, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27918477/identification-and-characterisation-of-the-antimicrobial-peptide-phylloseptin-pt-from-the-skin-secretion-of-phyllomedusa-tarsius-and-comparison-of-activity-with-designed-cationicity-enhanced-analogues-and-diastereomers
#5
Yitian Gao, Di Wu, Xinping Xi, Yue Wu, Chengbang Ma, Mei Zhou, Lei Wang, Mu Yang, Tianbao Chen, Chris Shaw
Antimicrobial peptides belonging to the phylloseptin family are mainly found in phyllomedusine frogs. These peptides not only possess potent antimicrobial activity but exhibit low toxicity against eukaryotic cells. Therefore, they are considered as promising drug candidates for a number of diseases. In a recent study, potent antimicrobial activity was correlated with the conserved structures and cationic amphiphilic characteristics of members of this peptide family. A phylloseptin peptide precursor was discovered here in the skin secretion of Phyllomedusa tarsius and the mature peptide was validated by MS/MS sequencing, and was subsequently named phylloseptin-PT...
December 3, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27917887/13-methylberberine-a-berberine-analogue-with-stronger-anti-adipogenic-effects-on-mouse-3t3-l1-cells
#6
Yit-Lai Chow, Mami Sogame, Fumihiko Sato
Lipid metabolism modulation is a main focus of metabolic syndrome research, an area in which many natural and synthetic chemicals are constantly being screened for in vitro and in vivo activity. Berberine, a benzylisoquinoline plant alkaloid, has been extensively investigated for its anti-obesity effects and as a potential cholesterol and triglyceride-lowering drug. We screened 11 protoberberine and 2 benzophenanthridine alkaloids for their anti-adipogenic effects on 3T3-L1 adipocytes and found that 13-methylberberine exhibited the most potent activity...
December 5, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27917846/knowledge-and-attitudes-of-physicians-and-pharmacists-towards-the-use-of-generic-medicines-in-bosnia-and-herzegovina
#7
Tarik Čatić, Lejla Avdagić, Igor Martinović
Aim To investigate and assess knowledge and attitudes of pharmacists and physicians towards generic drugs prescription in order to evaluate current trends, obstacles to prescribe/dispense generics and suggest possible improvements of rational and economic prescribing having in mind scarce public budgets for drugs. Methods A cross-sectional survey among 450 primary care physicians (prescribers) and pharmacists in four major cities in Bosnia and Herzegovina (Sarajevo, Banja Luka, Tuzla and Mostar) during the period between January and March 2016 was conducted...
February 1, 2017: Medicinski Glasnik
https://www.readbyqxmd.com/read/27917615/design-synthesis-and-evaluation-of-2-9-bis-substituted-aminomethyl-phenyl-1-10-phenanthroline-derivatives-as-g-quadruplex-ligands
#8
Nassima Meriem Gueddouda, Miyanou Rosales Hurtado, Stéphane Moreau, Luisa Ronga, Rabindra Nath Das, Solène Savrimoutou, Sandra Rubio, Adrien Marchand, Oscar Mendoza, Mathieu Marchivie, Lilian Elmi, Albain Chansavang, Vanessa Desplat, Valérie Gabelica, Anne Bourdoncle, Jean-Louis Mergny, Jean Guillon
Genomic sequences able to form guanine quadruplexes (G4) are found in oncogene promoters, in telomeres and in 5' and 3' untranslated regions as well as introns of messenger RNAs. These regions are potential targets for drugs designed to treat cancer. In the present work, we present the design and syntheses of ten new phenantroline derivatives and characterization of their interactions with G4-forming oligonucleotides. We evaluated ligand-induced stabilization and specificity and selectivity of ligands for various G4 conformations using FRET-melting experiments...
December 4, 2016: ChemMedChem
https://www.readbyqxmd.com/read/27916836/expression-purification-and-characterization-of-interleukin-11-orthologues
#9
Andrei S Sokolov, Alexei S Kazakov, Valery V Solovyev, Ramis G Ismailov, Vladimir N Uversky, Yulia S Lapteva, Roman V Mikhailov, Ekaterina V Pavlova, Iana O Terletskaya, Ludmila V Ermolina, Sergei E Permyakov, Eugene A Permyakov
Interleukin-11 (IL-11) is a multifunctional cytokine implicated in several normal and pathological processes. The decoding of IL-11 function and development of IL-11-targeted drugs dictate the use of laboratory animals and need of the better understanding of species specificity of IL-11 signaling. Here, we present a method for the recombinant interleukin-11 (rIL-11) production from the important model animals, mouse and macaque. The purified mouse and macaque rIL-11 interact with extracellular domain of human IL-11 receptor subunit α and activate STAT3 signaling in HEK293 cells co-expressing human IL-11 receptors with efficacies resembling those of human rIL-11...
November 29, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/27916566/extracellular-vesicle-mimetics-novel-alternatives-to-extracellular-vesicle-based-theranostics-drug-delivery-and-vaccines
#10
REVIEW
Oh Youn Kim, Jaewook Lee, Yong Song Gho
Extracellular vesicles are nano-sized spherical bilayered proteolipids encasing various components. Cells of all domains of life actively release these vesicles to the surroundings including various biological fluids. These extracellular vesicles are known to play pivotal roles in numerous pathophysiological functions. Extracellular vesicles have distinct characteristics, like high biocompatibility, safety, and nano-sized diameters that allow efficient drug loading capacity and long blood circulation half-life...
December 1, 2016: Seminars in Cell & Developmental Biology
https://www.readbyqxmd.com/read/27914299/the-effects-of-fluorine-substitution-on-the-chemical-properties-and-inhibitory-capacity-of-donepezil-anti-alzheimer-drug-density-functional-theory-and-molecular-docking-calculations
#11
Azita Khosravan, Safora Marani, Mohammad Sadegh Sadeghi Googheri
Drug fluorination has the potential to reproduce useful drugs with decreasing the side effect of them. Identifying the effect of this improvement on the chemical properties and biological interactions of drug symbolizes a meaningful progress in drug design. Here the fluorination of Donepezil as an anti-Alzheimer drug, including 7 fluorinated derivatives of it, was investigated computationally. In the first part of our calculations, the most important chemical properties of drug that affects the drug efficiency were investigated by applying the M06/6-31g (d, p) and M062X/6-31g (d, p) levels of theories...
November 25, 2016: Journal of Molecular Graphics & Modelling
https://www.readbyqxmd.com/read/27913416/mutagenesis-of-nosm-leader-peptide-reveals-important-elements-in-nosiheptide-biosynthesis
#12
Liang Jin, Xuri Wu, Yanjiu Xue, Yue Jin, Shuzhen Wang, Yijun Chen
: Nosiheptide, a typical member of ribosomally synthesized and post-translationally modified peptides (RiPPs), exhibits potent activity against multi-drug resistant Gram-positive bacterial pathogens. The precursor peptide of nosiheptide (NosM) is comprised of a leader peptide with 37 amino acids and a core peptide containing 13 amino acids. To pinpoint essential elements in the leader peptide for nosithpetide biosynthesis, a collection of mutants with unique sequence features, including N- and C-terminal motifs, peptide length as well as specific sites in the leader peptide, was generated by mutagenesis in vivo The effects of various mutants on nosiheptide biosynthesis were evaluated...
December 2, 2016: Applied and Environmental Microbiology
https://www.readbyqxmd.com/read/27912884/synergism-of-coumarins-from-the-chinese-drug-zanthoxylum-nitidum-with-antibacterial-agents-against-methicillin-resistant-staphylococcus-aureus-mrsa
#13
Guo-Ying Zuo, Chun-Juan Wang, Jun Han, Yu-Qing Li, Gen-Chun Wang
BACKGROUND: Methicillin-resistant Staphylococcus aureus (MRSA) poses a serious therapeutic challenge in current clinic and new drug development. Natural coumarins have diverse bioactivities and the potential of resistance modifying effects. PURPOSE: This study is to present in-depth evaluations of in vitro antimicrobial activities of four natural coumarins 5-geranyloxy-7-methoxycoumarin (Gm, 1), (5,7-dimethoxy-8-prenyloxycoumarin (artanin, Ar, 2)), isopimpinellin (Is, 3) and phellopterin (Ph, 4) from Zanthoxylum nitidum (Roxb...
December 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/27911675/on-safety-margin-for-drug-interchangeability
#14
Jiayin Zheng, Shein-Chung Chow, Fuyu Song
As more and more generic (or biosimilar) drug products become available in the market place, it is a concern whether the approved generic (or biosimilar) drug products are safe and efficacious and hence can be used interchangeably. According to current regulation, most regulatory agencies such as the United States Food and Drug Administration (FDA) indicate an approved generic (or biosimilar) drug product can serve as a substitute for the innovative drug product. Bioequivalence (biosimilarity) assessment for regulatory approval among generic copies (or biosimilars) of the innovative drug product are not required...
December 2, 2016: Journal of Biopharmaceutical Statistics
https://www.readbyqxmd.com/read/27910176/visible-light-accelerated-c-h-sulfinylation-of-heteroarenes
#15
Andreas Uwe Meyer, Alexander Wimmer, Burkhard König
Heteroaromatic sulfoxides are a frequent structural motif in natural products, drugs, catalysts, and materials. We report a metal-free visible-light-accelerated synthesis of heteroaromatic sulfoxides from sulfinamides and peroxodisulfate. The reaction proceeds at room temperature with blue-light irradiation and allows the C-H sulfinylation of electron-rich heteroarenes, such as pyrroles and indoles. An electrophilic aromatic substitution mechanism is proposed based on the substrate scope, substitution selectivity, and competition experiments with different nucleophiles...
December 2, 2016: Angewandte Chemie
https://www.readbyqxmd.com/read/27908808/emergency-hybrid-approach-to-ruptured-femoral-pseudoaneurysm-in-hiv-positive-intravenous-drug-abusers
#16
Maurizio Domanin, Giovanni Romagnoni, Silvia Romagnoli, Antonio Rolli, Livio Gabrielli
PURPOSE: Chronic traumatism of the common femoral artery due to intravenous injection in drug abusers, in association with local infections and arterial wall weakening caused by HIV, can lead to the development of pseudoaneurysms. Rupture of pseudoaneurysm is a dramatic event in such patients and its correction is difficult and controversial. Most of the cases reported describe open surgical elective options, that consist in ligation, repair or substitution of the damaged arterial segment, employing when possible biological grafts...
November 28, 2016: Annals of Vascular Surgery
https://www.readbyqxmd.com/read/27908757/synthesis-antioxidant-and-antichagasic-properties-of-a-selected-series-of-hydroxy-3-arylcoumarins
#17
Natalia Robledo-O'Ryan, Maria João Matos, Saleta Vazquez-Rodriguez, Lourdes Santana, Eugenio Uriarte, Mauricio Moncada-Basualto, Francisco Mura, Michel Lapier, Juan Diego Maya, Claudio Olea-Azar
Oxidative stress is involved in several parasitic diseases such as Chagas. Agents able to selectively modulate biochemical processes involved in the disease represent promising multifunctional agents for the delay or abolishment of the progression of this pathology. In the current work, differently substituted hydroxy-3-arylcoumarins are described, exerting both antioxidant and trypanocidal activity. Among the compounds synthesized, compound 8 showed the most interesting profile, presenting a moderate scavenging ability for peroxyl radicals (ORAC-FL=2...
November 19, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27907875/s-substituted-3-5-dinitrophenyl-1-3-4-oxadiazole-2-thiols-and-tetrazole-5-thiols-as-highly-efficient-antitubercular-agents
#18
Galina Karabanovich, Jan Němeček, Lenka Valášková, Alejandro Carazo, Klára Konečná, Jiřina Stolaříková, Alexandr Hrabálek, Oto Pavliš, Petr Pávek, Kateřina Vávrová, Jaroslav Roh, Věra Klimešová
Two new classes of antitubercular agents, namely 5-alkylsulfanyl-1-(3,5-dinitrophenyl)-1H-tetrazoles and 2-alkylsulfanyl-5-(3,5-dinitrophenyl)-1,3,4-oxadiazoles, and their structure-activity relationships are described. These compounds possessed excellent activity against Mycobacterium tuberculosis, including the clinically isolated multidrug (MDR) and extensively drug-resistant (XDR) strains, with no cross resistance with first or second-line anti-TB drugs. The minimum inhibitory concentration (MIC) values of the most promising compounds reached 0...
November 21, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27907087/prenylated-polyphenols-from-clusiaceae-and-calophyllaceae-with-immunomodulatory-activity-on-endothelial-cells
#19
Caroline Rouger, Sylvain Pagie, Séverine Derbré, Anne-Marie Le Ray, Pascal Richomme, Béatrice Charreau
Endothelial cells (ECs) are key players in inflammation and immune responses involved in numerous pathologies. Although attempts were experimentally undertaken to prevent and control EC activation, drug leads and probes still remain necessary. Natural products (NPs) from Clusiaceous and Calophyllaceous plants were previously reported as potential candidates to prevent endothelial dysfunction. The present study aimed to identify more precisely the molecular scaffolds that could limit EC activation. Here, 13 polyphenols belonging to 5 different chemical types of secondary metabolites (i...
2016: PloS One
https://www.readbyqxmd.com/read/27902737/a-comparison-of-the-sensititre-mycotb-plate-the-bactec-mgit-960-and-a-microarray-based-molecular-assay-for-the-detection-of-drug-resistance-in-clinical-mycobacterium-tuberculosis-isolates-in-moscow-russia
#20
Elena Y Nosova, Danila V Zimenkov, Anastasia A Khakhalina, Alexandra I Isakova, Ludmila Y Krylova, Marina V Makarova, Ksenia Y Galkina, Maria A Krasnova, Svetlana G Safonova, Vitaly I Litvinov, Dmitry A Gryadunov, Elena M Bogorodskaya
BACKGROUND: The goal of this study was to compare the consistency of three assays for the determination of the drug resistance of Mycobacterium tuberculosis (MTB) strains with various resistance profiles isolated from the Moscow region. METHODS: A total of 144 MTB clinical isolates with a strong bias toward drug resistance were examined using Bactec MGIT 960, Sensititre MycoTB, and a microarray-based molecular assay TB-TEST to detect substitutions in the rpoB, katG, inhA, ahpC, gyrA, gyrB, rrs, eis, and embB genes that are associated with resistance to rifampin, isoniazid, fluoroquinolones, second-line injectable drugs and ethambutol...
2016: PloS One
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