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https://www.readbyqxmd.com/read/28231522/novel-2-3-disubstituted-quinazoline-4-3h-one-molecules-derived-from-amino-acid-linked-sulphonamide-as-a-potent-malarial-antifolates-for-dhfr-inhibition
#1
Tarosh S Patel, Satish F Vanparia, Urmila H Patel, Ritu B Dixit, Chaitanya J Chudasama, Bhavesh D Patel, Bharat C Dixit
An optimization of a modified Grimmel's method for N-heterocyclization of Leucine linked sulphonamide leading to 2,3-disustituted-4-quinazolin-(3H)-ones was accomplished. Further, nineteen hybrid quinazolinone motifs (5a-5s) were synthesized by N-heterocyclization reaction under microwave irradiation using TEAA (IL) as green solvent as well as catalyst. The in vitro screening of the hybrid entities against the plasmodium species P. falciparum yielded five antimalarial potent molecules 5g, 5l, 5m, 5n &5p owing comparable activity to the reference drugs...
February 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28231494/marijuana-and-other-substance-use-among-male-and-female-underage-drinkers-who-drive-after-drinking-and-ride-with-those-who-drive-after-drinking
#2
Lisa Buckley, Erin E Bonar, Maureen A Walton, Patrick M Carter, Diana Voloshyna, Peter F Ehrlich, Rebecca M Cunningham
The study sought to describe the occurrence of adolescent driving after drinking (DD) and riding with a driver who had been drinking (RWDD) and associations with substance use for both males and females. As part of screening for a randomized controlled trial, we surveyed 16-20year olds (N=3418) recruited from an emergency department (ED) and analyzed data from those reporting past-year alcohol consumption (n=2150, 58% females). DD was reported by 22% of females and 28% of males and RWDD was reported by 39% of females and 38% of males, also in the past year...
February 10, 2017: Addictive Behaviors
https://www.readbyqxmd.com/read/28231380/perioperative-medications-for-preventing-temporarily-increased-intraocular-pressure-after-laser-trabeculoplasty
#3
REVIEW
Linda Zhang, Jennifer S Weizer, David C Musch
BACKGROUND: Glaucoma is the international leading cause of irreversible blindness. Intraocular pressure (IOP) is the only currently known modifiable risk factor; it can be reduced by medications, incisional surgery, or laser trabeculoplasty (LTP). LTP reduces IOP by 25% to 30% from baseline, but early acute IOP elevation after LTP is a common adverse effect. Most of these IOP elevations are transient, but temporarily elevated IOP may cause further optic nerve damage, worsening of glaucoma requiring additional therapy, and permanent vision loss...
February 23, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28231062/relationship-between-metabolic-phenotypes-and-genotypes-of-cyp1a2-and-cyp2a6-in-the-nigerian-population
#4
Ayorinde Adehin, Oluseye O Bolaji, Simran Maggo, Martin A Kennedy
BACKGROUND: CYP1A2 and CYP2A6 are polymorphic drug-metabolising enzymes that are also implicated in the activation of procarcinogens in humans. Some of their alleles and haplotypes, often varied in prevalence across populations, are thought to influence activity despite the known contribution of environmental factors. This study assessed the potential influence of some genetic variants of CYP1A2 and CYP2A6 on metabolic phenotypes in Nigerians. METHODS: Genomic DNA was extracted from blood samples of 100 healthy, unrelated subjects for whom CYP1A2 and CYP2A6 phenotypes had previously been determined, alongside an additional 80 other individuals for whom phenotype data were unavailable...
February 23, 2017: Drug Metabolism and Personalized Therapy
https://www.readbyqxmd.com/read/28231034/upscaling-of-hips-cell-derived-neurons-for-high-throughput-screening
#5
Stefanie Traub, Heiko Stahl, Holger Rosenbrock, Eric Simon, Ralf Heilker
The advent of human-induced pluripotent stem (hiPS) cell-derived neurons promised to provide better model cells for drug discovery in the context of the central nervous system. This work demonstrates both the upscaling of cellular expansion and the acceleration of neuronal differentiation to accommodate the immense material needs of a high-throughput screening (HTS) approach. Using GRowth factor-driven expansion and INhibition of NotCH (GRINCH) during maturation, the derived cells are here referred to as GRINCH neurons...
March 2017: SLAS Discov
https://www.readbyqxmd.com/read/28230985/discovery-of-competitive-and-non-competitive-ligands-of-the-organic-cation-transporter-1-oct1-slc22a1
#6
Eugene C Chen, Natalia Khuri, Xiaomin Liang, Adrian Stecula, Huan-Chieh Chien, Sook Wah Yee, Yong Huang, Andrej Sali, Kathleen M Giacomini
Organic cation transporter 1 (OCT1) plays a critical role in the hepatocellular uptake of structurally diverse endogenous compounds and xenobiotics. Here, we identified competitive and noncompetitive OCT1 interacting ligands in a library of 1,780 prescription drugs by combining in silico and in vitro methods. Ligands were predicted by docking against a comparative model based a eukaryotic homolog. In parallel, high-throughput screening (HTS) was conducted using the fluorescent probe substrate ASP+ in cells overexpressing human OCT1...
February 23, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28230762/the-development-of-ck2-inhibitors-from-traditional-pharmacology-to-in-silico-rational-drug-design
#7
REVIEW
Giorgio Cozza
Casein kinase II (CK2) is an ubiquitous and pleiotropic serine/threonine protein kinase able to phosphorylate hundreds of substrates. Being implicated in several human diseases, from neurodegeneration to cancer, the biological roles of CK2 have been intensively studied. Upregulation of CK2 has been shown to be critical to tumor progression, making this kinase an attractive target for cancer therapy. Several CK2 inhibitors have been developed so far, the first being discovered by "trial and error testing". In the last decade, the development of in silico rational drug design has prompted the discovery, de novo design and optimization of several CK2 inhibitors, active in the low nanomolar range...
February 20, 2017: Pharmaceuticals
https://www.readbyqxmd.com/read/28230579/hospital-outpatient-visits-associated-with-medication-related-problems-in-thailand-a-multicenter-prospective-observational-study
#8
Supinya Dechanont, Arom Jedsadayanmata, Bodin Butthum, Chuenjid Kongkaew
OBJECTIVES: The aims of the study were to investigate the prevalence of hospital visits associated with medication-related problems (MRPs, i.e., adverse drug events [ADEs], adverse drug reactions [ADRs], nonadherence [NA] to medication, and medication error) and to identify the medications involved in hospital visits associated with MRPs in outpatient departments (OPDs). METHODS: A prospective observational study was carried out in OPD of 11 hospitals in the lower northern region of Thailand...
February 22, 2017: Journal of Patient Safety
https://www.readbyqxmd.com/read/28230562/chronic-hepatitis-c-and-individuals-with-a-history-of-injecting-drugs-in-spain-population-assessment-challenges-for-successful-treatment
#9
Carlos Roncero, Richard Littlewood, Pablo Vega, Jose Martinez-Raga, Marta Torrens
In Spain, there is a need to improve chronic hepatitis C care among people who inject drugs (PWID). Injecting drug use is an important risk behaviour for hepatitis C virus (HCV) infection. Review of 28 sources of the relevant published literature mapped the size of the addiction-HCV population in Spain. Experts in opioid use disorder (OUD) treatment in Spain completed a consensus to define the population size, HCV prevalence and access or barriers to hepatitis C treatment for PWID populations. In Spain, over 300 000 individuals have a lifetime history of injecting drugs...
February 22, 2017: European Journal of Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/28229367/inhibition-of-mtor-pathway-by-rapamycin-decreases-p-glycoprotein-expression-and-spontaneous-seizures-in-pharmacoresistant-epilepsy
#10
Xiaosa Chi, Cheng Huang, Rui Li, Wei Wang, Mengqian Wu, Jinmei Li, Dong Zhou
The mammalian target of rapamycin (mTOR) has been demonstrated to mediate multidrug resistance in various tumors by inducing P-glycoprotein (P-gp) overexpression. Here, we investigated the correlation between the mTOR pathway and P-gp expression in pharmacoresistant epilepsy. Temporal cortex specimens were obtained from patients with refractory mesial temporal lobe epilepsy (mTLE) and age-matched controls who underwent surgeries at West China Hospital of Sichuan University between June 2014 and May 2015. We established a rat model of epilepsy kindled by coriaria lactone (CL) and screened pharmacoresistant rats (non-responders) using phenytoin...
February 22, 2017: Journal of Molecular Neuroscience: MN
https://www.readbyqxmd.com/read/28228650/haematopoietic-stem-cell-transplantation-for-autoimmune-diseases
#11
REVIEW
Joost F Swart, Eveline M Delemarre, Femke van Wijk, Jaap-Jan Boelens, Jürgen Kuball, Jacob M van Laar, Nico M Wulffraat
Autologous haematopoietic stem cell transplantation (HSCT) is the only treatment that is able to induce long-term, drug-free and symptom-free remission in several refractory autoimmune rheumatic diseases. Over 3,000 HSCT procedures for rheumatic and nonrheumatic severe autoimmune diseases have been performed worldwide. Specific conditioning regimens are currently used to eradicate the autoreactive immunological memory of patients. Although in vivo immune cell depletion with antithymocyte globulin or anti-CD52 is the norm for many regimens, ex vivo selection of CD34(+) stem cells from the graft is controversial...
February 23, 2017: Nature Reviews. Rheumatology
https://www.readbyqxmd.com/read/28228617/silkworm-fungal-infection-model-for-identification-of-virulence-genes-in-pathogenic-fungus-and-screening-of-novel-antifungal-drugs
#12
Masaki Ishii, Yasuhiko Matsumoto, Ikuko Nakamura, Kazuhisa Sekimizu
The silkworm infection model has the potential to replace conventional animal models for evaluation of the efficacy and toxicity of investigational antifungal agents. Silkworms are relatively inexpensive, can be simply grown in large numbers and can be easily infected with pathogenic fungi, including mutant strains. Antifungal agents can then be injected into the silkworm either via the hemolymph to mimic intravenous administration or directly into the gut for oral administration, and their antifungal effect can be evaluated...
February 21, 2017: Drug Discoveries & Therapeutics
https://www.readbyqxmd.com/read/28228097/alkaloid-extracts-from-combretum-zeyheri-inhibit-the-growth-of-mycobacterium-smegmatis
#13
Tafadzwa Nyambuya, Ruvimbo Mautsa, Stanley Mukanganyama
BACKGROUND: Current tuberculosis regimens have failed to combat the issue of drug resistance and ethno medicines may represent a possible source of antimycobacterial agents. Combretum species are well known in African traditional medicines and used for various ailments including pneumonia, venereal diseases like syphilis, mental problems, relief of sore throats and colds, fever, and chest coughs associated with tuberculosis. Alkaloids function as either hydrogen-acceptor or hydrogen-donor in hydrogen bonding critical for the interaction between targets thus, potentiating effects of curative agents on diseases...
February 23, 2017: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#14
Golla Madhava, Katla Venkata Ramana, Saddala Madhu Sudhana, Devineni Subba Rao, Kuntrapakam Hema Kumar, Valluru Lokanatha, Asupatri Usha Rani, Chamarthi Naga Raju
BACKGROUND: Cyclooxygenase (COX-2) inhibitors have been developed to provide better anti-inflammatory and analgesic efficacy than those of traditional NSAIDs. Several compounds having selective COX-2 inhibitors such as SC-558, Celecoxib, Rofecoxib, Valdecoxib and Etoricoxib are marketed as new generation NSAIDs and block the production of prostaglandins (PGs) in inflammatory cells. New anti-inflammatory dynamic agents with improved potency and safety profile are still needed. OBJECTIVE: As a part of our continuation research work towards the synthesis of anti-inflammatory agents, the synthesis of N-substituted aryl/heteroaryl-pyrazole-1yl benzene sulfonamide (Celecoxib) derivatives, and evaluated their anti-inflammatory activity in both methods in vitro and in vivo, and molecular docking study on COX-2 enzyme will be discussed in this study...
February 20, 2017: Medicinal Chemistry
https://www.readbyqxmd.com/read/28227912/a-hybrid-discrete-continuous-model-of-in-vitro-spheroid-tumor-growth-and-drug-response
#15
Giorgos Tzedakis, Evangelos Liapis, Eleftheria Tzamali, Giannis Zacharakis, Vangelis Sakkalis, Giorgos Tzedakis, Evangelos Liapis, Eleftheria Tzamali, Giannis Zacharakis, Vangelis Sakkalis, Giannis Zacharakis, Vangelis Sakkalis, Evangelos Liapis, Giorgos Tzedakis, Eleftheria Tzamali
Anti-cancer therapy efficacy in solid tumors mainly depends on drug transportation through the vasculature system and the extracellular matrix, on diffusion gradients and clonal heterogeneity within the tumor mass, as well as on the responses of the individual tumor cells to drugs and their interactions with each other and their local microenvironment. In this work, we develop a mathematical predictive model for tumor growth and drug response based on 3D spheroids experiments that possess several in vivo features of tumors and are considered better for drug screening...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28227815/lab-on-chips-for-manipulation-of-small-scale-organisms-to-facilitate-imaging-of-neurons-and-organs
#16
Ramtin Ardeshiri, Pouya Rezai, Ramtin Ardeshiri, Pouya Rezai, Ramtin Ardeshiri, Pouya Rezai
Caenorhabditis elegans (C. elegans) and Drosophila melanogaster (D. melanogaster) are widely-used model organisms for neurological and cardiac studies due to their simple neuronal (302 neurons in C. elegans) and cardiac (simple tubular organ in D. melanogaster) systems. However, their small sizes and continuous mobility impede their precise and timely manipulation, hence, limiting the assays that can be done using conventional manual methods. This has resulted in a need for technologies that allow multidirectional manipulation of model organisms to enable studies on target neurons and organs throughout the body...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28227433/microprinted-tumor-spheroids-enable-anti-cancer-drug-screening
#17
Pradip S Thakuri, Stephanie L Ham, Hossein Tavana, Pradip S Thakuri, Stephanie L Ham, Hossein Tavana, Stephanie L Ham, Hossein Tavana
Spheroids present a biologically relevant model of avascular tumors and a unique tool for discovery of anti-cancer drugs. Despite being used in research laboratories for several decades, spheroids are not routinely used for drug discovery primarily due to the difficulty of mass-producing uniformly-sized spheroids and intense labor involved in handling, drug treatment, and analyzing them. We overcome this barrier using a novel technology to robotically microprint spheroids in standard 384-well plates. An aqueous drop containing cancer cells is dispensed into a bath of a second, immiscible aqueous phase...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28226865/electrical-resistance-increases-at-the-tissue-electrode-interface-as-an-early-response-to-nucleus-accumbens-deep-brain-stimulation
#18
Rajas P Kale, Abbas Z Kouzani, Julian Berk, Ken Walder, Michael Berk, Susannah J Tye, Rajas P Kale, Abbas Z Kouzani, Julian Berk, Ken Walder, Michael Berk, Susannah J Tye, Julian Berk, Michael Berk, Susannah J Tye, Abbas Z Kouzani, Rajas P Kale, Ken Walder
The therapeutic actions of deep brain stimulation are not fully understood. The early inflammatory response of electrode implantation is associated with symptom relief without electrical stimulation, but is negated by anti-inflammatory drugs. Early excitotoxic necrosis and subsequent glial scarring modulate the conductivity of the tissue-electrode interface, which can provide some detail into the inflammatory response of individual patients. The feasibility of this was demonstrated by measuring resistance values across a bipolar electrode which was unilaterally implanted into the nucleus accumbens of a rat while receiving continuous deep brain stimulation with a portable back-mounted device using clinical parameters (130Hz, 200μA, 90μs) for 3 days...
August 2016: Conference Proceedings: Annual International Conference of the IEEE Engineering in Medicine and Biology Society
https://www.readbyqxmd.com/read/28226337/immunoassay-based-drug-tests-are-inadequately-sensitive-for-medication-compliance-monitoring-in-patients-treated-for-chronic-pain
#19
Marion L Snyder, Corrine R Fantz, Stacy Melanson
BACKGROUND: Enzyme immunoassays (EIA) have notable limitations for monitoring therapeutic compliance in pain management. Chromatography coupled with mass spectrometry provides definitive results and superior sensitivity and specificity over traditional EIA testing. OBJECTIVE: To analyze and compare the sensitivity of EIA results together with known prescriptions to liquid chromatography-tandem mass spectrometry (LC-MS/MS) for monitoring drug use (and abuse) in patients treated for chronic pain...
February 2017: Pain Physician
https://www.readbyqxmd.com/read/28226335/repeated-quantitative-urine-toxicology-analysis-may-improve-chronic-pain-patient-compliance-with-opioid-therapy
#20
Nebojsa Nick Knezevic, Omar M Khan, Afsaneh Beiranvand, Kenneth D Candido
BACKGROUND: Even though serious efforts have been undertaken by different medical societies to reduce opioid use for treating chronic benign pain, many Americans continue to seek pain relief through opioid consumption. Assuring compliance of these patients may be a difficult aspect of proper management even with regular behavioral monitoring. OBJECTIVE: The purpose of this study was to accurately assess the compliance of chronic opioid-consuming patients in an outpatient setting and evaluate if utilizing repeated urine drug testing (UDT) could improve compliance...
February 2017: Pain Physician
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