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https://www.readbyqxmd.com/read/28351081/osteoarthritis-patients-experiences-of-pharmacotherapy-for-pain-management-in-iran-a-qualitative-study
#1
Vahid Zamanzadeh, Fazlollah Ahmadi, Mozhgan Behshid, Alireza Irajpoor, Parvin Zakeri-Milani
Despite the effectiveness of pharmacotherapy for pain management in patients with osteoarthritis (OA), personal biases in the selection, administration, and continuation of pharmacotherapy challenge the proper management of symptoms and the effectiveness of the therapy. This study was conducted to carry out an in-depth examination of the experiences of patients with OA about their use of pharmacotherapy for the OA pain management and the existing challenges. The present qualitative study was conducted on 17 patients with OA, 5 of their family members and 8 healthcare personnel using a conventional content analysis approach...
March 28, 2017: Drug Research
https://www.readbyqxmd.com/read/28346364/new-benzimidazole-1-2-4-triazole-hybrid-compounds-synthesis-anticandidal-activity-and-cytotoxicity-evaluation
#2
Hülya Karaca Gençer, Ulviye Acar Çevik, Serkan Levent, Begüm Nurpelin Sağlık, Büşra Korkut, Yusuf Özkay, Sinem Ilgın, Yusuf Öztürk
Owing to the growing need for antifungal agents, we synthesized a new series 2-((5-(4-(5-substituted-1H-benzimidazol-2-yl)phenyl)-4-substituted-4H-1,2,4-triazol-3-yl)thio)-1-(substitutedphenyl)ethan-1-one derivatives, which were tested against Candida species. The synthesized compounds were characterized and elucidated by FT-IR, ¹H-NMR, (13)C-NMR and HR-MS spectroscopies. The synthesized compounds were screened in vitro anticandidal activity against Candida species by broth microdiluation methods. In vitro cytotoxic effects of the final compounds were determined by MTT assay...
March 27, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28345866/biocompatible-hydroxylated-boron-nitride-nanosheets-polyvinyl-alcohol-interpenetrating-hydrogels-with-enhanced-mechanical-and-thermal-responses
#3
Lin Jing, Hongling Li, Roland Yingjie Tay, Bo Sun, Siu Hon Tsang, Olivier Cometto, Jinjun Lin, Edwin Hang Tong Teo, Alfred Iing Yoong Tok
Polyvinyl alcohol (PVA) hydrogels with tissue-like viscoelasticity, excellent biocompatibility and high hydrophilicity have been considered as promising cartilage replacement materials. However, lack of sufficient mechanical properties is a critical barrier to their usage as load-bearing cartilage substitutes. Herein, we report hydroxylated boron nitride nanosheets (OH-BNNS)/PVA interpenetrating hydrogels by cyclically freezing/thawing the aqueous mixture of PVA and highly hydrophilic OH-BNNS (up to 0.6 mg/mL, two times the highest reported so far)...
March 27, 2017: ACS Nano
https://www.readbyqxmd.com/read/28345306/the-burden-and-management-of-cytochrome-p450-2d6-cyp2d6-mediated-drug-drug-interaction-ddi-co-medication-of-metoprolol-and-paroxetine-or-fluoxetine-in-the-elderly
#4
Muh Akbar Bahar, Eelko Hak, Jens H J Bos, Sander D Borgsteede, Bob Wilffert
PURPOSE: Metoprolol and paroxetine/fluoxetine are inevitably co-prescribed because cardiovascular disorders and depression often coexist in the elderly. This leads to CYP2D6-mediated drug-drug interactions (DDI). Because systematic evaluations are lacking, we assessed the burden of metoprolol-paroxetine/fluoxetine interaction in the elderly and how these interactions are managed in Dutch community pharmacies. METHOD: Dispensing data were collected from the University of Groningen pharmacy database (IADB...
March 26, 2017: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/28345206/treatment-with-direct-acting-antiviral-agents-of-hepatitis-c-virus-infection-in-injecting-drug-users-a-prospective-study
#5
Lucio Boglione, Simone Mornese Pinna, Amedeo De Nicolò, Jessica Cusato, Giuseppe Cariti, Giovanni Di Perri, Antonio D'Avolio
In this prospective study, we evaluated the effectiveness and tolerability of novel therapies against hepatitis C virus (HCV) in a cohort of PWID enrolled at our centre from April 2015 to July 2016. In this analysis, a total of 174 patients were included: 11 (6.3%) were treated with pegylated-interferon (PEG-IFN) and ribavirin (RBV) containing regimens, 163 (93.7%) with IFN-free treatments. RBV has been used in 70 patients (40.2%); 59 (33.9%) patients were in opioid substitution therapy (OST) with methadone or buprenorphine...
March 26, 2017: Journal of Viral Hepatitis
https://www.readbyqxmd.com/read/28343771/characterization-of-human-monoclonal-antibodies-that-neutralize-multiple-poliovirus-serotypes
#6
Rama Devudu Puligedda, Diana Kouiavskaia, Fetweh H Al-Saleem, Chandana Devi Kattala, Usman Nabi, Hamid Yaqoob, V Sandeep Bhagavathula, Rashmi Sharma, Konstantin Chumakov, Scott K Dessain
Following the eradication of wild poliovirus (PV), achieving and maintaining a polio-free status will require eliminating potentially pathogenic PV strains derived from the oral attenuated vaccine. For this purpose, a combination of non-cross-resistant drugs, such as small molecules and neutralizing monoclonal antibodies (mAbs), may be ideal. We previously isolated chimpanzee and human mAbs capable of neutralizing multiple PV types (cross-neutralization). Here, we describe three additional human mAbs that neutralize types 1 and 2 PV and one mAb that neutralizes all three types...
March 23, 2017: Vaccine
https://www.readbyqxmd.com/read/28341945/translational-value-of-drug-discrimination-with-typical-and-atypical-antipsychotic-drugs
#7
Joseph H Porter, Kevin A Webster, Adam J Prus
This chapter focuses on the translational value of drug discrimination as a preclinical assay for drug development. In particular, the importance of two factors, i.e., training dose and species, for drug discrimination studies with the atypical antipsychotic clozapine is examined. Serotonin receptors appear to be an important pharmacological mechanism mediating clozapine's discriminative cue in both rats and mice, although differences are clearly evident as antagonism of cholinergic muscarinic receptors is important in rats at a higher training dose (5...
March 25, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28341944/discriminative-stimulus-effects-of-psychostimulants
#8
Michael D Berquist, William E Fantegrossi
Numerous drugs elicit locomotor stimulant effects at appropriate doses; however, we typically reserve the term psychostimulant to refer to drugs with affinity for monoamine reuptake transporters. This chapter comprises select experiments that have characterized the discriminative stimulus effects of psychostimulants using drug discrimination procedures. The substitution profiles of psychostimulants in laboratory rodents are generally consistent with those observed in human and nonhuman primate drug discrimination experiments...
March 25, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28341123/acetaminophen-analog-but-not-reactive-metabolite-induces-cyp3a-activity-via-inhibition-of-protein-degradation
#9
Masataka Santoh, Seigo Sanoh, Yuya Ohtsuki, Yoko Ejiri, Yaichiro Kotake, Shigeru Ohta
Cytochrome P450 (CYP) 3A subfamily members are known to metabolize various types of drugs, highlighting the importance of understanding drug-drug interactions (DDI) depending on CYP3A induction or inhibition. While transcriptional regulation of CYP3A members is widely understood, post-translational regulation needs to be elucidated. We previously reported that acetaminophen (APAP) induces CYP3A activity via inhibition of protein degradation and proposed a novel DDI concept. N-Acetyl-p-benzoquinone imine (NAPQI), the reactive metabolite of APAP formed by CYP, is known to cause adverse events related to depletion of intracellular reduced glutathione (GSH)...
March 21, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28340419/photolytic-degradation-of-the-%C3%AE-blocker-nebivolol-in-aqueous-solution
#10
Alaa Salma, Holger V Lutze, Torsten C Schmidt, Jochen Tuerk
Nebivolol (NEB) is one of the top-sold prescription drugs belonging to the third generation of beta-blockers. However, so far, occurrence data in the environment are lacking. Within this study NEB has been found for the first time in effluent samples of wastewater treatment plants in Germany with an average concentration of 13 ng L(-1). Its photodegradation behavior in the environment and in technical processes is largely unknown. To fill this gap, three different UV treatment procedures (UV-C at 254 nm, UV-B at 312 nm and UV-A at 365 nm) were investigated in three different matrices: pure water, pure water in presence of the hydroxyl radical (OH) scavenger tert...
March 13, 2017: Water Research
https://www.readbyqxmd.com/read/28338602/design-and-synthesis-of-novel-pyrazole-substituted-different-nitrogenous-heterocyclic-ring-systems-as-potential-anti-inflammatory-agents
#11
Eman S Nossier, Hoda H Fahmy, Nagy M Khalifa, Wafaa I El-Eraky, Marawan A Baset
With the aim of developing novel anti-inflammatory scaffolds, a new series of pyrazole-substituted various nitrogenous heterocyclic ring systems at C-4 position were synthesized through different chemical reactions and validated by means of spectral and elemental data. The new obtained compounds were investigated for their anti-inflammatory activity using the carrageenan-induced paw edema standard technique and revealed that, compound 6b showed increased potency with % inhibition of edema 85.23 ± 1.92 and 85...
March 24, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28337317/structural-requirements-of-hdac-inhibitors-saha-analogues-modified-at-the-c2-position-display-hdac6-8-selectivity
#12
Ahmed T Negmeldin, Geetha Padige, Anton V Bieliauskas, Mary Kay H Pflum
Histone deacetylase (HDAC) proteins are epigenetic regulators that deacetylate protein substrates, leading to subsequent changes in cell function. HDAC proteins are implicated in cancers, and several HDAC inhibitors have been approved by the FDA as anticancer drugs, including SAHA (suberoylanilide hydroxamic acid; Vorinostat and Zolinza). Unfortunately, SAHA inhibits most HDAC isoforms, which limits its use as a pharmacological tool and may lead to side effects in the clinic. In this work SAHA analogues substituted at the C2 position were synthesized and screened for HDAC isoform selectivity in vitro and in cells...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28335293/cholesterol-modified-amino-pullulan-nanoparticles-as-a-drug-carrier-comparative-study-of-cholesterol-modified-carboxyethyl-pullulan-and-pullulan-nanoparticles
#13
Xiaojun Tao, Yongchao Xie, Qiufang Zhang, Ximin Qiu, Liming Yuan, Yi Wen, Min Li, Xiaoping Yang, Ting Tao, Minghui Xie, Yanwei Lv, Qinyi Wang, Xing Feng
To search for nano-drug preparations with high efficiency in tumor treatment, we evaluated the drug-loading capacity and cell-uptake toxicity of three kinds of nanoparticles (NPs). Pullulan was grafted with ethylenediamine and hydrophobic groups to form hydrophobic cholesterol-modified amino-pullulan (CHAP) conjugates. Fourier transform infrared spectroscopy and nuclear magnetic resonance were used to identify the CHAP structure and calculate the degree of substitution of the cholesterol group. We compared three types of NPs with close cholesterol hydrophobic properties: CHAP, cholesterol-modified pullulan (CHP), and cholesterol-modified carboxylethylpullulan (CHCP), with the degree of substitution of cholesterol of 2...
September 8, 2016: Nanomaterials
https://www.readbyqxmd.com/read/28334702/in-vitro-antibacterial-activity-of-7-substituted-6-fluoroquinolone-and-7-substituted-6-8-difluoroquinolone-derivatives
#14
Socorro Leyva-Ramos, Denisse de Loera, Jaime Cardoso-Ortiz
BACKGROUND: Fluoroquinolones are widely prescribed synthetic antimicrobial agents. Quinolones act by converting their targets, gyrase and topoisomerase IV, into toxic enzymes that fragment the bacterial chromosome; the irreversible DNA damage eventually causes the killing of bacteria. Thorough knowledge of the structure-activity relationship of quinolones is essential for the development of new drugs with improved activity against resistant strains. METHODS: The compounds were screened for their antibacterial activity against 4 representing strains using the Kirby-Bauer disk diffusion method...
March 24, 2017: Chemotherapy
https://www.readbyqxmd.com/read/28333118/synthesis-of-novel-saccharin-derivatives
#15
Gregory M Rankin, Sally-Ann Poulsen
The synthesis of saccharin (1,2-benzisothiazol-3-one-1,1-dioxide) derivatives substituted on the benzene ring has seen limited development despite the longevity of this compound's use as an artificial sweetener. This type of saccharin derivative would however present attractive properties for the development of new bioactive, drug-like small molecule compounds. Here we report the derivatisation of the benzene ring of saccharin using Cu(I)-catalyzed azide alkyne cycloaddition (CuAAC) to synthesise a diverse library of novel saccharin-1,2,3-triazole conjugates...
March 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28332824/indole-substituted-benzothiazoles-and-benzoxazoles-as-selective-and-reversible-mao-b-inhibitors-for-treatment-of-parkinson-s-disease
#16
Min-Ho Nam, Moosung Park, Hyeri Park, Youngjae Kim, Seulki Yoon, Vikram Shahaji Sawant, Ji Won Choi, Jong-Hyun Park, Ki Duk Park, Sun-Joon Min, Changjoon Justin Lee, Hyunah Choo
To develop a novel, selective, and reversible MAO-B inhibitors for safer treatment of Parkinson's disease, benzothiazole and benzoxazole derivatives with indole moiety were designed and synthesized. Most of the synthesized compounds showed inhibitory activities against MAO-B and selectivity over MAO-A. The most active compound was Compound 5b, 6-fluoro-2-(1-methyl-1H-indol-5-yl)benzo[d]thiazole with an IC50 value of 29 nM with no apparent effect on MAO-A activity at 10 M. Based on the reversibility assay, Compound 5b turned out to be a fully reversible with over 95% of recovery of enzyme activity after washout of the compound...
March 23, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28331841/resistance-testing-for-the-treatment-of-chronic-hepatitis-c-with-direct-acting-antivirals-when-and-for-how-long
#17
Ana Belén Pérez, Natalia Chueca, Federico García
The need to test for resistance associated substitutions (RAS) has been intensively debated in the past two years. In the absence of pangenotypic combinations, it seems reasonable that, if available, RAS testing in the NS5A gene at baseline for genotypes 1a and 3 may help to avoid overtreatment in terms of ribavirin usage and/or prolonged treatment duration. When patients fail treatment, RAS testing may also be useful to guide the selection of the new regimen, especially for those that need urgent retreatment and that have failed a combination including an NS5A inhibitor...
March 2017: Germs
https://www.readbyqxmd.com/read/28331637/mode-of-delivery-in-drug-dependent-pregnant-women-a-case-control-study
#18
Ana Raquel Neves, Fabiane Neves, Isabel Santos Silva, Maria do Céu Almeida, Pitorra Monteiro
Objective. To determine the contribution of drug use during pregnancy to the route of delivery. Methods. A case-control study was conducted at a hospital in Coimbra, Portugal, between 2001 and 2014. Drug-dependent pregnant women (n = 236) were compared with a control group of low risk women (n = 228) in terms of maternal characteristics, obstetric history, pregnancy complications, and labor details. Factors that influenced the mode of delivery were determined. Statistical analysis was performed with SPSS v...
2017: Journal of Pregnancy
https://www.readbyqxmd.com/read/28330089/discovery-of-potential-alk-inhibitors-by-virtual-screening-approach
#19
Anish Kumar, V Shanthi, K Ramanathan
Crizotinib is an anticancer drug used for the treatment of non-small cell lung cancer. Evidences available suggest that there is a development of an acquired resistance against crizotinib action due to the emergence of several mutations in the ALK gene. It is therefore necessary to develop potent anti-cancer drugs for the treatment of crizotinib resistance non-small cell lung cancer types. In the present study, a novel class of lead molecule was identified using virtual screening, molecular docking and molecular dynamic approach...
June 2016: 3 Biotech
https://www.readbyqxmd.com/read/28326640/catalytic-enantioselective-synthesis-of-protecting-group-free-1-5-benzothiazepines
#20
Sara Meninno, Chiara Volpe, Alessandra Lattanzi
A one-pot enantioselective route to N-unprotected 2,3-dihydro-1,5-benzothiazepinones, by an organocatalyzed sulfa-Michael reaction of readily available α,β-unsaturated N-acyl pyrazoles with 2-aminothiophenols followed by silica-gel-catalyzed lactamization, has been developed. The method proceeds under mild conditions at room temperature and it requires only 1 mol % catalyst loading, to give 2-aryl/alkyl-substituted 1,5-benzothiazepines in generally good to excellent yields and enantioselectivities. The process, used for a short synthesis of antidepressant drug (R)-(-)-thiazesim, represents the first method to access enantioenriched unprotected 1,5-benzotiazepines, which are useful for rapid derivatization in drug discovery...
March 22, 2017: Chemistry: a European Journal
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