keyword
MENU ▼
Read by QxMD icon Read
search

drug substitution

keyword
https://www.readbyqxmd.com/read/28103180/fluoroquinolone-macrolide-and-ketolide-resistance-in-haemophilus-parainfluenzae-from-south-africa
#1
Regina Esinam Abotsi, Usha Govinden, Krishnee Moodley, Sabiha Essack
Fluoroquinolones and ketolides are among the drugs of choice for the treatment of Haemophilus parainfluenzae infections. There has been a report of an emerging fluoroquinolone and telithromycin resistance in H. parainfluenzae isolates from the private sector of KwaZulu-Natal Province of South Africa that necessitates molecular investigation. The aim of this study is to characterize these resistance delineating mutations in genes commonly associated with reduced susceptibility. Ten H. parainfluenzae isolates retrieved from the sputum of 10 patients with H...
January 19, 2017: Microbial Drug Resistance: MDR: Mechanisms, Epidemiology, and Disease
https://www.readbyqxmd.com/read/28101955/prescription-drug-monitoring-programs-produce-a-limited-impact-on-painkiller-prescribing-in-medicare-part-d
#2
Courtney R Yarbrough
OBJECTIVE: To measure the impact of prescription drug monitoring programs (PDMPs) on prescribing of opioid and nonopioid painkillers. DATA SOURCE: 2010-2013 physician-level Medicare Part D prescribing data released by the Centers for Medicare and Medicaid Services and Propublica. STUDY DESIGN: Using difference-in-differences models with physician-level fixed effects, the study compares prescribing in states with and without PDMPs for opioid and nonopioid analgesics, oxycodone, hydrocodone, and opioids by controlled substances Schedules II-IV...
January 18, 2017: Health Services Research
https://www.readbyqxmd.com/read/28101253/2-chromon-3-yl-imidazole-derivatives-as-potential-antimicrobial-agents-synthesis-biological-evaluation-and-molecular-docking-studies
#3
Shweta Sharma, Vishal Sharma, Gurpreet Singh, Harpreet Kaur, Shubham Srivastava, Mohan Paul S Ishar
A series of novel 2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (4a-h) were synthesized by one pot condensation of substituted 3-formylchromones (1a-h), benzil (2) and ammonium acetate (3) in refluxing acetic acid at 110 °C under N2 atmosphere. Allylation of compounds 4a-h with allyl bromide in the presence of fused K2CO3 furnished N-allyl-2-(chromon-3-yl)-4,5-diphenyl-1H-imidazoles (6a-h). The synthesized compounds were characterized spectroscopically and evaluated for in vitro antimicrobial activity against various pathogenic bacterial and fungal strains by disc diffusion method...
January 2017: Journal of Chemical Biology
https://www.readbyqxmd.com/read/28099089/genotypic-characterization-of-quinolone-resistant-escherichia-coli-isolates-from-retail-food-in-morocco
#4
Kaotar Nayme, Abouddihaj Barguigua, Brahim Bouchrif, Bouchra Karraouan, Fatima El Otmani, Naima Elmdaghri, Khalid Zerouali, Mohammed Timinouni
This study was conducted to assess the retail food as a possible vehicle for antimicrobial resistant, particularly quinolones resistant and pathogenic Escherichia coli. We determined the prevalence and characteristics of nalidixic acid (Nal) resistant E. coli isolates from diverse retail food samples. In all, 70 (28%) of 250 E. coli isolates studied were Nal-resistant E. coli and 91% of these were multi-drug resistant. Plasmid mediated quinolone resistance genes were identified in 32 isolates, including aac(6')-Ib-cr (n = 16), qnrS1 (n = 11) and qnrB19 (n = 7)...
February 2017: Journal of Environmental Science and Health. Part. B, Pesticides, Food Contaminants, and Agricultural Wastes
https://www.readbyqxmd.com/read/28098433/synthesis-and-evaluation-of-anti-inflammatory-n-substituted-3-5-bis-2-trifluoromethyl-benzylidene-piperidin-4-ones
#5
Zixin Xie, Zaikui Zhang, Shufang Yu, Donghua Cheng, Huan Zhang, Chao Han, Handeng Lv, Faqing Ye
A total of 24 N-substituted 3,5-bis(2-(trifluoromethyl)benzylidene)piperidin-4-one derivatives were synthesized via aldol condensation, and their anti-inflammatory activities were evaluated. These compounds were found to have no significant cytotoxicity against mouse bone marrow cells in vitro. However, some compounds, such as c6 (N-(3-methylbenzoyl)-3,5-bis-(2-(trifluoromethyl)benzylidene)piperidin-4-one) and c10 (N-(2-chlorobenzoyl)-3,5-bis-(2-(trifluoromethyl)benzylidene)piperidin-4-one), displayed potent anti-inflammatory activity by inhibiting lipopolysaccharide (LPS)-stimulated tumor necrosis factor (TNF)-α, interleukin-6 (IL-6), IL-1β, prostaglandin E2 (PGE2), and nitric oxide (NO) production in RAW 264...
January 18, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28098422/structural-elucidation-of-a-non-peptidic-inhibitor-specific-for-the-human-immunoproteasome
#6
Haissi Cui, Regina Baur, Camille Le Chapelain, Christian Dubiella, Wolfgang Heinemeyer, Eva Maria Huber, Michael Groll
Selective inhibition of the immunoproteasome is a promising approach towards the development of immunomodulatory drugs. Recently, a class of substituted thiazole compounds that combine a non-peptidic scaffold with the absence of an electrophile has been reported in a patent. Herein, we describe the mode of action of the lead compound using a sophisticated chimeric yeast model of the human immunoproteasome for structural studies. The inhibitor adopts a unique orientation perpendicular to the β5i substrate binding channel...
January 18, 2017: Chembiochem: a European Journal of Chemical Biology
https://www.readbyqxmd.com/read/28094943/exploitation-of-a-multienzymatic-stereoselective-cascade-process-in-the-synthesis-of-2-methyl-3-substituted-tetrahydrofurans-precursors
#7
Elisabetta Brenna, Michele Crotti, Francesco Gilberto Gatti, Ludovico Marinoni, Daniela Monti, Sara Quaiato
Enantiopure 2-methyl-3-substituted tetrahydrofurans are key precursors of several biologically active products (drugs, flavors and agrochemicals). Thus, a stereocontrolled and efficient methodology for the obtainment of these synthons is highly desirable. We exploited a two-steps multienzymatic stereoselective cascade reduction of α-bromo-α,β-unsaturated ketones to give the corresponding bromohydrins in good yields, with high ee and de values. The cascade process is catalyzed by an ene-reductase and an alcohol dehydrogenase...
January 17, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28094550/pharmacophore-modelling-atom-based-3d-qsar-generation-and-virtual-screening-of-molecules-projected-for-mpges-1-inhibitory-activity
#8
S Misra, M Saini, H Ojha, D Sharma, K Sharma
COX-2 inhibitors exhibit anticancer effects in various cancer models but due to the adverse side effects associated with these inhibitors, targeting molecules downstream of COX-2 (such as mPGES-1) has been suggested. Even after calls for mPGES-1 inhibitor design, to date there are only a few published inhibitors targeting the enzyme and displaying anticancer activity. In the present study, we have deployed both ligand and structure-based drug design approaches to hunt novel drug-like candidates as mPGES-1 inhibitors...
January 17, 2017: SAR and QSAR in Environmental Research
https://www.readbyqxmd.com/read/28094219/3-4-dihydropyrimidinone-coumarin-analogues-as-a-new-class-of-selective-agent-against-s-aureus-synthesis-biological-evaluation-and-molecular-modelling-study
#9
Nirmala S Naik, Lokesh A Shastri, Shrinivas D Joshi, Sheshagiri R Dixit, Bahubali M Chougala, S Samundeeswari, Megharaj Holiyachi, Farzanabi Shaikh, Jyoti Madar, Rashmi Kulkarni, Vinay Sunagar
Bacterial infections are increasingly difficult to combat as bacteria evolve resistance to antibiotic drugs and have severely compromised the arsenal of antibiotic drugs. On the other hand matrix metalloproteinases (MMPs) play a fundamental role in inflammation and extracellular matrix degradation in physiological and pathological conditions. In search of potent antibiotic, taking coumarin and dihydropyrimidinone as lead compound, a green, eco-friendly and efficient protocol has been developed and synthesized the dihydropyrimidin-2(1H)-one/thione derivatives of coumarin 3/4 from substituted 4-formylcoumarins 2 and ethylacetoacetate using urea/thiourea in the presence of catalytic amount of ceric ammonium nitrate is reported...
January 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28093722/triptan-use-in-australia-1997-2015-a-pharmacoepidemiological-study
#10
B L K D Eyre, M J Eadie, M L van Driel, L Ross-Lee, S A Hollingworth
OBJECTIVE: This study examined the use of triptan derivatives in Australia between 1997 and 2015, based on a national drug reimbursement database, and compared patterns of use with available international data. METHODS: We obtained publically available data on the number of prescriptions for triptans marketed in Australia (sumatriptan, eletriptan, rizatriptan, zolmitriptan, naratriptan). Dispensed use was measured as defined daily dose (DDD per 1000 population per day) for Australia's concessional beneficiaries (low-income earners, people with disabilities, and seniors)...
January 16, 2017: Acta Neurologica Scandinavica
https://www.readbyqxmd.com/read/28093029/low-doses-of-mirtazapine-or-quetiapine-for-transient-insomnia-a-randomised-double-blind-cross-over-placebo-controlled-trial
#11
Julie Karsten, Loes A Hagenauw, Jeanine Kamphuis, Marike Lancel
Low doses of the antidepressant mirtazapine or the neuroleptic quetiapine are often prescribed off-label for insomnia. However, studies on the effects on sleep and hangover effects the following day are scarce. In this randomised, double-blind, cross-over, placebo-controlled trial, the influence of 7.5 mg mirtazapine and 50 mg quetiapine on both normal sleep and sleep disturbed by acoustic stress (traffic noise) as a model for transient insomnia was assessed. Additionally, hangover effects on next-day alertness and cognitive functioning were examined...
January 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28092111/design-and-synthesis-of-5-substituted-benzo-d-1-3-dioxole-derivatives-as-potent-anticonvulsant-agents
#12
Shiyang Dong, Tiantian Wang, Chundi Hu, Xiaodong Chen, Yi Jin, Zengtao Wang
A series of 5-substituted benzo[d][1,3]dioxole derivatives was designed, synthesized, and tested for anticonvulsant activity using the maximal electroshock (MES) and subcutaneous pentylenetetrazole (scPTZ) screens. Neurotoxicity was determined by rotarod test. In the preliminary screening, six compounds, 3a, 3c, 3d, and 4d-f, showed promising anticonvulsant activities in the MES model, and compounds 4c and 4d exhibited full protection against seizures at doses of 300 mg/kg in the scPTZ model. Among the synthesized compounds, 3c as the most active compound showed high protection against the MES-induced seizures with an ED50 value of 9...
January 16, 2017: Archiv der Pharmazie
https://www.readbyqxmd.com/read/28089942/targeting-egfr-t790m-mutation-in-nsclc-from-biology-to-evaluation-and-treatment
#13
Antonio Passaro, Elena Guerini-Rocco, Alessia Pochesci, Davide Vacirca, Gianluca Spitaleri, Chiara Matilde Catania, Alessandra Rappa, Massimo Barberis, Filippo de Marinis
The identification of EGFR mutations and their respectively tyrosine kinase inhibitors (TKIs), changed dramatically treatment and survival of patients with EGFR-positive lung cancer. Nowadays, different EGFR TKIs as afatinib, erlotinib and gefitinib are approved worldwide for the treatment of NSCLC harbouring EGFR mutations, in particular exon 19 deletions or exon 21 (Leu858Arg) substitution EGFR mutations. In first-line setting, when comparing with platinum-based chemotherapy, these target drugs improves progression-free survival, response rate and quality of life...
January 12, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28087785/thermolytic-degradation-of-synthetic-cannabinoids-chemical-exposures-and-pharmacological-consequences
#14
Brian F Thomas, Timothy W Lefever, Ricardo A Cortes, Alexander L Kovach, Anderson O Cox, Purvi R Patel, Gerald T Pollard, Julie A Marusich, Richard A Kevin, Thomas F Gamage, Jenny L Wiley
Synthetic cannabinoids are manufactured clandestinely with little quality control and are distributed as herbal "Spice" for smoking or as bulk compound for mixing with a solvent and inhalation via electronic vaporizers. Intoxication with synthetic cannabinoids has been associated with seizure, excited delirium, coma, kidney damage, and other disorders. The chemical alterations produced by heating these structurally novel compounds for consumption are largely unknown. Here we show that heating synthetic cannabinoids containing tetramethylcyclopropyl-ring substituents produced thermal degradants with pharmacological activity that varied considerably from their parent compounds...
January 13, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28086832/norcantharidin-inhibits-cell-growth-by-suppressing-the-expression-and-phosphorylation-of-both-egfr-and-c-met-in-human-colon-cancer-cells
#15
Peiju Qiu, Siwen Wang, Ming Liu, He Ma, Xuan Zeng, Meng Zhang, Lingling Xu, Yidi Cui, Huixin Xu, Yang Tang, Yanli He, Lijuan Zhang
BACKGROUND: Norcantharidin (NCTD) is a Chinese FDA approved, chemically synthesized drug for cancer treatment. The effect of NCTD on signaling proteins of EGFR and c-Met was systematically elucidated in current study. METHODS: Two human colon cancer cell lines, HCT116 and HT29, were used as model systems to investigate the anti-cancer molecular mechanism of NCTD. Cell cycle arrest and early/late apoptosis were analyzed by flow cytometry. The levels of EGFR, phospho-EGFR, c-Met, phospho-c-Met and other related proteins were quantified by western blot analysis...
January 13, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28081594/management-of-direct-antiviral-agent-failures
#16
REVIEW
María Buti, Rafael Esteban
The current standard of care for patients with chronic hepatitis C virus (HCV) infection is a combination of direct-acting antiviral agents (DAAs). Most HCV patients treated with these drugs achieve viral elimination, but 1% to 15% fail to attain this objective. Treatment failures are usually related to relapse, and less often to on-treatment viral breakthrough. HCV drug resistant associated substitutions are detected in most patients who do not eliminate the virus. The risk of developing these variants depends on host- and virus-related factors, the properties of the drugs used, and the treatment strategies applied...
December 2016: Clinical and Molecular Hepatology
https://www.readbyqxmd.com/read/28080146/perceptions-vs-evidence-therapeutic-substitutes-for-antipsychotics-in-patients-with-dementia-in-long-term-care
#17
Brianne L Olivieri-Mui, John W Devlin, Aileen Ochoa, Danielle Schenck, Becky Briesacher
OBJECTIVE: To compare differences between clinician perceptions of therapeutic substitutes for antipsychotics prescribed to patients with dementia in long term care (LTC) and published evidence. METHODS: A mixed-methods approach that included a drug information search, online survey of 55 LTC clinicians and a comprehensive literature review was used. For 41 pharmacologic antipsychotic substitute candidates identified, LTC clinicians rated the likelihood they would substitute each for patients with dementia and identified non-pharmacologic antipsychotic substitutes...
January 12, 2017: Aging & Mental Health
https://www.readbyqxmd.com/read/28080063/optimization-of-2-anilino-4-amino-substituted-quinazolines-into-potent-antimalarial-agents-with-oral-in-vivo-activity
#18
Paul R Gilson, Cyrus Tan, Kate E Jarman, Kym N Lowes, Joan M Curtis, William Nguyen, Adrian E Di Rago, Hayley E Bullen, Boris Prinz, Sandra Duffy, Jonathan B Baell, Craig A Hutton, Helene Jousset Sabroux, Brendan S Crabb, Vicky M Avery, Alan F Cowman, Brad E Sleebs
Novel antimalarial therapeutics that target multiple stages of the parasites lifecycle are urgently required to tackle the emerging problem of resistance with current drugs. Here we describe the optimization of the 2-anilino quinazoline class as antimalarial agents. The class, identified from publicly available antimalarial screening data, was optimized to generate lead compounds that possess potent antimalarial activity against P. falciparum parasites equivalent to the known antimalarials, chloroquine and mefloquine...
January 12, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28079305/gallium-enhances-reconstructive-properties-of-a-calcium-phosphate-bone-biomaterial
#19
Ivana Strazic Geljic, Nicolas Melis, Florian Boukhechba, Sébastien Schaub, Charlotte Mellier, Pascal Janvier, Jean-Pierre Laugier, Jean-Michel Bouler, Elise Verron, Jean-Claude Scimeca
Calcium phosphate-based (CaP) biomaterials are commonly used in bone reconstructive surgery to replace the damaged tissue, and can also serve as vectors for local drug delivery. Due to its inhibitory action on osteoclasts, the semi-metallic element gallium (Ga) is used for the systemic treatment of disorders associated with accelerated bone resorption. As it was demonstrated that Ga could be incorporated in the structure of CaP biomaterials, we investigated in the present work the biological properties of Ga-loaded CaP biomaterials...
January 12, 2017: Journal of Tissue Engineering and Regenerative Medicine
https://www.readbyqxmd.com/read/28077295/improved-mucoadhesive-properties-of-self-nanoemulsifying-drug-delivery-systems-snedds-by-introducing-acyl-chitosan
#20
Nuri Ari Efiana, Arshad Mahmood, Hung Thanh Lam, Ožbej Zupančič, Gintare Leonaviciute, Andreas Bernkop-Schnürch
This study was aimed to improve the mucoadhesive properties of SNEDDS by the incorporation of acyl chitosan including octanoyl chitosan (OC), lauroyl chitosan (LC) and palmitoyl chitosan (PC). SNEDDS and acyl chitosan SNEDDS were characterized regarding droplet size and zeta potential. Their mucoadhesivity on porcine intestinal mucosa was evaluated by falling liquid film technique using Sudan Red G as marker. Degree of substitution of chitosan was determined to be 52.8%, 64.8 and 48.5% for OC, LC and PC, respectively...
January 8, 2017: International Journal of Pharmaceutics
keyword
keyword
38903
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"