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https://www.readbyqxmd.com/read/28231439/the-rights-of-drug-treatment-patients-experience-of-addiction-treatment-in-poland-from-a-human-rights-perspective
#1
Justyna Klingemann
BACKGROUND: Drug dependence is a recognized medical condition and therefore, right to health applies in the same way to drug dependence as it does to any other health condition. The human rights in patient care framework - which refers to the application of basic human rights principles in the delivery of health care services - was used to explore the experiences of equality in the dignity and rights protected by Polish law within four different specialist drug treatment settings in Poland...
February 20, 2017: International Journal on Drug Policy
https://www.readbyqxmd.com/read/28230972/paclitaxel-biosynthesis-adenylation-and-thiolation-domains-of-an-nrps-tyca-pheat-module-produce-various-arylisoserine-coa-thioesters
#2
Ruth Muchiri, Kevin D Walker
Structure-activity relationship studies show that the phenylisoserinyl moiety of paclitaxel is largely necessary for the effective anticancer activity. Several paclitaxel analogs with a variant isoserinyl sides chain have improved pharmaceutical properties over the parent drug. To produce the isoserinyl CoAs as intermediates needed for enzyme catalysis on a semibiosynthetic pathway to paclitaxel analogs, we repurposed the adenylation and thiolation domains of a non-ribosomal peptide synthetase (Phe-AT) to function as a CoA ligase...
February 23, 2017: Biochemistry
https://www.readbyqxmd.com/read/28230776/effects-and-side-effects-of-using-sorafenib-and-sunitinib-in-the-treatment-of-metastatic-renal-cell-carcinoma
#3
REVIEW
Caroline Randrup Hansen, Daniela Grimm, Johann Bauer, Markus Wehland, Nils E Magnusson
In recent years, targeted therapies have proven beneficial in terms of progression-free survival (PFS) and overall survival (OS) in the treatment of metastatic renal cell carcinoma (mRCC). The tyrosine kinase inhibitors (TKIs) sorafenib and sunitinib are included in international clinical guidelines as first-line and second-line therapy in mRCC. Hypertension is an adverse effect of these drugs and the degree of hypertension associates with the anti-tumour effect. Studies have compared newer targeted drugs to sorafenib and sunitinib in terms of PFS, OS, quality of life and safety profiles...
February 21, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28229435/design-and-pharmacodynamics-of-recombinant-nz2114-histidine-mutants-with-improved-activity-against-methicillin-resistant-staphylococcus-aureus
#4
Huixian Chen, Ruoyu Mao, Da Teng, Xiumin Wang, Ya Hao, Xingjun Feng, Jianhua Wang
NZ2114 is a promising candidate for therapeutic application owing to its potent activity to Staphylococcus aureus. Our objective was to identify NZ2114 derivatives with improved activity through substitution of His16 and His18 with residues Arginine and Lysine. Eight mutants were designed and expressed in Pichia pastoris X-33 via pPICZαA. Five of them exhibited strong antimicrobial activity against S. aureus at low minimal inhibitory concentrations (MICs) of 0.057-0.454 μM. Among them, H1, H2, and H3 showed ideal pharmacodynamic effects on methicillin-resistant S...
December 2017: AMB Express
https://www.readbyqxmd.com/read/28228362/development-of-mbri-001-a-deuterium-substituted-plinabulin-derivative-as-a-potent-anti-cancer-agent
#5
Zhongpeng Ding, Hejuan Cheng, Shixiao Wang, Yingwei Hou, Jianchun Zhao, Huashi Guan, Wenbao Li
Plinabulin, a drug targeting microtubule of cancer cells, has been currently tried in its phase III clinical study. However, low efficacy caused by poor pharmacokinetic (PK) properties has been considered to be the main obstacle to approved by the Food and Drug Administration. Herein, we introduced a deuterium atom as an isostere in its structure to become a new compound named (MBRI-001, No. 9 in a series of deuterium-substituted compounds). The structure of MBRI-001 was characterized by HRMS, NMR, IR and a single crystal analysis...
February 3, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28228088/aryl-heteroaryl-substituted-celecoxib-derivatives-as-cox-2-inhibitors-synthesis-anti-inflammatory-activity-and-molecular-docking-studies
#6
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/28225629/synthesis-of-fluorenones-from-benzaldehydes-and-aryl-iodides-dual-c-h-functionalizations-using-a-transient-directing-group
#7
Xiao-Yang Chen, Seyma Ozturk, Erik J Sorensen
The first synthesis of substituted fluorenones directly from benzaldehydes and aryl iodides via a Pd(II)-catalyzed C(sp(2))-H functionalization cascade is reported. Featuring anthranilic acid as an inexpensive transient directing group, the process is compatible with a variety of benzaldehydes and aryl iodides. A three-step synthesis of the antiviral drug Tilorone was completed in an excellent overall yield (40%), demonstrating the utility of this method.
February 22, 2017: Organic Letters
https://www.readbyqxmd.com/read/28225601/rational-optimization-of-diphenyl-ether-binding-kinetics-to-the-enoyl-acp-reductase-fabi1-from-burkholderia-pseudomallei
#8
Carla Maya Neckles, Sandra Eltschkner, Jason Ellsworth Cummings, Maria Hirschbeck, Fereidoon Daryaee, Gopal R Bommineni, Zhuo Zhang, Lauren A Spagnuolo, Weixuan Yu, Shabnam Davoodi, Richard A Slayden, Caroline Kisker, Peter J Tonge
There is growing awareness of the link between drug-target residence time and in vivo drug activity, and there are increasing efforts to determine the molecular factors that control the lifetime of a drug-target complex. Rational alterations in drug-target residence time require knowledge of both the ground and transition states on the inhibition reaction coordinate, and we have determined the structure-kinetic relationship for 22 ethyl or hexyl substituted diphenyl ethers that are slow-binding inhibitors of bpFabI1, the enoyl-ACP reductase FabI1 from Burkholderia pseudomallei...
February 22, 2017: Biochemistry
https://www.readbyqxmd.com/read/28225570/washless-method-enables-multilayer-coating-of-an-aggregation-prone-nanoparticulate-drug-delivery-system-with-enhanced-yields-colloidal-stability-and-scalability
#9
Lamees Nayef, Rafael Castiello, Maryam Tabrizian
Aggregation is frequently encountered during coating nanoparticles, especially when the core is not solid and the coating polyelectrolytes are weak. Here, the coating of a nanoliposome with two weak polyelectrolytes, alginate and chitosan, is investigated. First, quartz crystal microbalance with dissipation, atomic force microscopy, scanning electron microscopy, and energy dispersive spectroscopy analyses confirm the feasibility of firm adsorption of up to 16 layers of weak polyelectrolytes to the liposomal surface...
February 22, 2017: Macromolecular Bioscience
https://www.readbyqxmd.com/read/28224884/water-soluble-co-polyelectrolytes-by-selective-modification-of-cellulose-esters
#10
Shu Liu, Kevin J Edgar
Cellulose-based materials are well-suited for biomedical uses, because of their abundance, renewable nature, biodegradability, and relatively low cost. However, the set of commercially available cellulose esters and ethers is limited in number and diversity, and contains no cationically charged cellulose esters. Herein we report a simple, efficient strategy for synthesizing cationic, water-soluble co-polyelectrolytes from commercial, hydrophobic, renewable-based cellulose esters. Cellulose acetate (degree of substitution (DS) 1...
April 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28223864/clinical-pharmacist-interventions-in-refill-clinic-at-tertiary-care-eye-specialist-hospital
#11
Sitah N Alzuman, Abdullah S Al-Humaidan
Objective: To describe the role of Clinical Pharmacists in the Medication Refill Clinic area as a part of a multidisciplinary team in which he/she can provide education to patients and caregivers on the safe and appropriate use of medications, counsel on medication compliance, monitor and manage medication side effects, as well as screen for dangerous drug interactions. Methods: The data of this prospective, single-centered, chart review based study have been collected since the clinic launched in June 2011 till December 2013 in King Khalid Eye Specialist Hospital which is a Tertiary Hospital in KSA...
January 2017: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/28223393/novel-bacterial-topoisomerase-inhibitors-with-potent-broad-spectrum-activity-against-drug-resistant-bacteria
#12
Cédric Charrier, Anne-Marie Salisbury, Victoria J Savage, Thomas Duffy, Emmanuel Moyo, Nathan Chaffer-Malam, Nicola Ooi, Rebecca Newman, Jonathan Cheung, Richard Metzger, David McGarry, Mark Pichowicz, Ralph Sigerson, Ian R Cooper, Gary Nelson, Hayley S Butler, Mark Craighead, Andrew J Ratcliffe, Stuart A Best, Neil R Stokes
The Novel Bacterial Topoisomerase Inhibitor class is an investigational type of antibacterial inhibitor of DNA gyrase and topoisomerase IV that do not have cross-resistance with the quinolones. Here, we report the evaluation of the in vitro properties of a new series of this type of small molecules. Exemplar compounds selectively and potently inhibited the catalytic activities of Escherichia coli DNA gyrase and topoisomerase IV but did not block the DNA breakage-reunion step. Compounds showed broad-spectrum inhibitory activity against a wide range of Gram-positive and Gram-negative pathogens, including biodefence microorganisms, and Mycobacterium tuberculosis No cross-resistance with quinolone-resistant Staphylococcus aureus and E...
February 21, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28222362/quinazolinone-benzimidazole-conjugates-synthesis-characterization-dihydrofolate-reductase-inhibition-dna-and-protein-binding-properties
#13
Prinka Singla, Vijay Luxami, Kamaldeep Paul
Quinazolinone and benzimidazole represent as important and abundant classes of fused nitrogen-containing heterocycle. A series of two isomeric quinazolinone-benzimidazole conjugates is synthesized and substitutes with different aromatic rings. These compounds are well characterized by (1)H and (13)C NMR as well as mass spectrometry. Compounds are then evaluated by dihydrofolate reductase inhibitory activity. In vitro assay shows that some compounds are exhibiting significant dihydrofolate reductase inhibitory activities...
February 14, 2017: Journal of Photochemistry and Photobiology. B, Biology
https://www.readbyqxmd.com/read/28221250/factors-associated-with-discontinuation-of-anti-tnf-inhibitors-among-persons-with-ibd-a-population-based-analysis
#14
Laura E Targownik, Aruni Tennakoon, Stella Leung, Lisa M Lix, Zoann Nugent, Harminder Singh, Charles N Bernstein
INTRODUCTION: Antitumor necrosis factor (anti-TNF) medications are known to be highly efficacious in persons with moderate-to-severe inflammatory bowel disease (IBD). There is a paucity of data from population-based sources to elucidate persistence with these medications in the general population of IBD. Discontinuation of anti-TNF therapy is a marker of lack of effectiveness, intolerance, and patient/physician practice preferences. METHODS: We identified all persons with IBD in Manitoba who were dispensed infliximab (IFX) and adalimumab (ADA) between 2001 and 2014...
March 2017: Inflammatory Bowel Diseases
https://www.readbyqxmd.com/read/28220863/engineering-botulinum-neurotoxin-c1-as-a-molecular-vehicle-for-intra-neuronal-drug-delivery
#15
Edwin J Vazquez-Cintron, Phillip H Beske, Luis Tenezaca, Bao Q Tran, Jonathan M Oyler, Elliot J Glotfelty, Christopher A Angeles, Aurelia Syngkon, Jean Mukherjee, Suzanne R Kalb, Philip A Band, Patrick M McNutt, Charles B Shoemaker, Konstantin Ichtchenko
Botulinum neurotoxin (BoNT) binds to and internalizes its light chain into presynaptic compartments with exquisite specificity. While the native toxin is extremely lethal, bioengineering of BoNT has the potential to eliminate toxicity without disrupting neuron-specific targeting, thereby creating a molecular vehicle capable of delivering therapeutic cargo into the neuronal cytosol. Building upon previous work, we have developed an atoxic derivative (ad) of BoNT/C1 through rationally designed amino acid substitutions in the metalloprotease domain of wild type (wt) BoNT/C1...
February 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28220862/induction-of-hair-follicle-dermal-papilla-cell-properties-in-human-induced-pluripotent-stem-cell-derived-multipotent-lngfr-thy-1-mesenchymal-cells
#16
Ophelia Veraitch, Yo Mabuchi, Yumi Matsuzaki, Takashi Sasaki, Hironobu Okuno, Aki Tsukashima, Masayuki Amagai, Hideyuki Okano, Manabu Ohyama
The dermal papilla (DP) is a specialised mesenchymal component of the hair follicle (HF) that plays key roles in HF morphogenesis and regeneration. Current technical difficulties in preparing trichogenic human DP cells could be overcome by the use of highly proliferative and plastic human induced pluripotent stem cells (hiPSCs). In this study, hiPSCs were differentiated into induced mesenchymal cells (iMCs) with a bone marrow stromal cell phenotype. A highly proliferative and plastic LNGFR(+)THY-1(+) subset of iMCs was subsequently programmed using retinoic acid and DP cell activating culture medium to acquire DP properties...
February 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28220706/human-cannabinoid-receptor-2-ligand-interaction-motif-transmembrane-helix-2-cysteine-c2-59-89-as-determinant-of-classical-cannabinoid-agonist-activity-and-binding-pose
#17
Han Zhou, Yan Peng, Aneetha Halikhedkar, Pusheng Fan, David R Janero, Ganesh A Thakur, Richard Warren Mercier, Xin Sun, Xiaoyu Ma, Alexandros Makriyannis
Cannabinoid receptor 2 (CB2R)-dependent signaling is implicated in neuronal physiology and immune surveillance by brain microglia. Selective CB2R agonists hold therapeutic promise for inflammatory and other neurological disorders. Information on human CB2R (hCB2R) ligand-binding and functional domains is needed to inform the rational design and optimization of candidate drug-like hCB2R agonists. Prior demonstration that hCB2R transmembrane helix 2 (TMH2) cysteine C2.59(89) reacts with small-molecule methanethiosulfonates showed that this cysteine residue is accessible to sulfhydryl derivatization reagents...
February 21, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28220474/buprenorphine-for-managing-opioid-withdrawal
#18
REVIEW
Linda Gowing, Robert Ali, Jason M White, Dalitso Mbewe
BACKGROUND: Managed withdrawal is a necessary step prior to drug-free treatment or as the endpoint of substitution treatment. OBJECTIVES: To assess the effects of buprenorphine versus tapered doses of methadone, alpha2-adrenergic agonists, symptomatic medications or placebo, or different buprenorphine regimens for managing opioid withdrawal, in terms of the intensity of the withdrawal syndrome experienced, duration and completion of treatment, and adverse effects...
February 21, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28220276/taxonomic-examination-of-longgu-fossilia-ossis-mastodi-dragon-bone-and-a-related-crude-drug-longchi-dens-draconis-dragon-tooth-from-japanese-and-chinese-crude-drug-markets
#19
Kazuki Oguri, Yuichiro Nishioka, Yoshitsugu Kobayashi, Kyoko Takahashi
Longgu ("dragon bone," Ryu-kotsu, Fossilia Ossis Mastodi, or Os Draconis) is the only fossil crude drug listed in the Japanese Pharmacopoeia. All longgu in the current Japanese market is imported from China, where its resources are being depleted. Therefore, effective countermeasures are urgently needed to prevent resource depletion. One possible solution is the development of a substitute made from bones of contemporary animals that are closely related to the original animal source of the current longgu. However, no research has been conducted on the original animal source of longgu, except for a report on the longgu specimens present in the Shosoin Repository...
February 20, 2017: Journal of Natural Medicines
https://www.readbyqxmd.com/read/28219202/-precision-treatment-after-resistance-to-first-generation-egfr-tki-in-patients-with-non-small-cell-lung-cancer
#20
C Pi, Y C Zhang, C R Xu, Q Zhou
Recently, with the research progress in molecular classification, the treatment of advanced non-small cell lung cancer (NSCLC) has been established as a model of anti-tumor treatment of precision medicine. The discovery of epidermal growth factor receptor-tyrosine kinase inhibitors (EGFR-TKI) has transformed the treatment of NSCLC from platinum based doublet chemotherapy into era of target therapy. EGFR-TKI, such as erlotinib and gefitinib, have been recommended as standard first-line treatment of patients with EGFR mutation...
February 23, 2017: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
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