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https://www.readbyqxmd.com/read/29161777/structure-based-design-and-evaluation-of-synthetic-porphyrin-derivatives-as-g-quadruplex-stabilizing-anticancer-agents
#1
R N Bhadane, D B Meshram, R M Gilhotra
G-quadruplex structures formed in telomeres and proto-oncogene represent a potentially useful target for anticancer drugs. Stabilization of this arrangement may inhibit the further action of different enzymes involved in cancer cell immortalization. In present work structure based drug design and synthesis was carried out on series of meso-substituted porphyrin analogues. The interaction of porphyrin derivatives with G-quadruplex DNA has been explored by virtual screening procedure. Some of the potential binding agents were then synthesized and evaluated in-vitro by MTT and PCR stop assay...
November 2017: Journal of Experimental Therapeutics & Oncology
https://www.readbyqxmd.com/read/29161629/the-effects-of-felbamate-on-appetitive-and-aversive-instrumental-learning-in-adult-rats
#2
John J Orczyk, Preston E Garraghty
Antiepileptic medications are the frontline treatment for seizure conditions but are not without cognitive side effects. Previously, our laboratory reported learning deficits in phenytoin-, carbamazepine-, and valproate-treated rats. In the present experiment, the effects of felbamate (FBM) have been compared to water-treated controls (controls) using the same instrumental training tasks employed here. Rats treated with FBM displayed a deficit in acquiring a tone-signaled avoidance response, relative to controls, but this was true only if they had no prior appetitive experience...
November 18, 2017: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/29161509/variation-in-the-supersaturation-and-phase-behavior-of-ezetimibe-amorphous-solid-dispersions-upon-dissolution-in-different-biorelevant-media
#3
Ahmed Elkhabaz, Sreya Sarkar, Janny K Dinh, Garth J Simpson, Lynne S Taylor
The delivery of poorly water-soluble drugs using amorphous solid dispersions (ASDs) has been widely acknowledged as a promising strategy for enhancing oral bioavailability. Upon dissolution, ASDs have accelerated dissolution rates and yield supersaturated solutions leading to higher apparent solubilities. Understanding the complex phase behavior of ASDs during dissolution is crucial for developing an effective formulation. Since the absorption of a lipophilic, high permeability drug is determined primarily by the intraluminal dissolution process and the final concentration achieved, there is a need for evaluation in biorelevant dissolution media that simulate both fasting and fed gastrointestinal states...
November 21, 2017: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29161395/postoperative-cognitive-dysfunction-and-dementia-what-we-need-to-know-and-do
#4
M J Needham, C E Webb, D C Bryden
Approximately 12% of apparently previously cognitively well patients undergoing anaesthesia and noncardiac surgery will develop symptoms of cognitive dysfunction after their procedure. Recent articles in this Journal have highlighted the difficulties of confirming any clear links between anaesthesia and cognitive dysfunction, in part because of the lack of consistency regarding definition and diagnosis. Postoperative cognitive dysfunction (POCD) is usually self-limiting and rarely persists in the longer term, although plausible biological mechanisms for an impact on brain protein deposition do exist...
December 1, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29161028/exploring-the-active-centre-of-lsd1-corest-complex-by-molecular-dynamics-simulation-utilizing-its-co-crystallized-cofactor-tetrahydrofolate-as-a-probe
#5
Waleed A A Zalloum, Hiba M Zalloum
Epigenetic targeting of cancer is a recent era to manipulate the gene without destroying the genetic material. Lysine-specific demethylase 1 (LSD1) is one of the enzymes associated with the chromatin for post-translational modifications, where it demethylates lysine amino acid in the chromatin H3 tail. Many studies showed that inhibiting LSD1 could potentially be used to treat cancer epigenetically. LSD1 is associated with its corepressor protein CoREST, and uses tetrahydrofolate as a cofactor to accept CH2 from the demethylation process...
November 21, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29161011/the-design-of-plasmodium-vivax-hypoxanthine-guanine-phosphoribosyltransferase-inhibitors-as-potential-antimalarial-therapeutics
#6
Dianne T Keough, Dominik Rejman, Radek Pohl, Eva Zborníková, Dana Hockova, Tristan Croll, Michael D Edstein, Geoff W Birrell, Marina Chavchich, Lieve M J Naesens, Gregory K Pierens, Ian M Brereton, Luke W Guddat
Plasmodium falciparum (Pf) and Plasmodium vivax (Pv) are the foremost causative agents of malaria. Due to the development of resistance to current antimalarial medications, new drugs for this parasitic disease need to be discovered. The activity of hypoxanthine-guanine-[xanthine]-phosphoribosyltransferase, HG[X]PRT, is reported to be essential for the growth of both of these parasites, making it an excellent target for antimalarial drug discovery. Here, we have used rational structure-based methods to design an inhibitor, [3R,4R]-4-guanin-9-yl-3-((S)-2-hydroxy-2-phosphonoethyl)oxy-1-N-(phosphonopropionyl)pyrrolidine, of PvHGPRT and PfHGXPRT which has Ki values of 8 nM and 7 nM, respectively for these two enzymes...
November 21, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/29161006/top-dnj-a-selective-inhibitor-of-endoplasmic-reticulum-%C3%AE-glucosidase-ii-exhibiting-anti-flaviviral-activity
#7
J L Kiappes, Michelle L Hill, Dominic S Alonzi, Joanna L Miller, Ren Iwaki, Andrew C Sayce, Alessandro T Caputo, Atsushi Kato, Nicole Zitzmann
Iminosugars have therapeutic potential against a range of diseases, due to their efficacy as glycosidase inhibitors. A major challenge in the development of iminosugar drugs lies in making a compound that is selective for the glycosidase associated with a given disease. We report the synthesis of ToP-DNJ, an antiviral iminosugar-tocopherol conjugate. Tocopherol was incorporated into the design of the iminosugar in order to direct the drug to the liver and immune cells, specific tissues of interest for antiviral therapy...
November 21, 2017: ACS Chemical Biology
https://www.readbyqxmd.com/read/29160839/inkjet-printing-of-drug-loaded-mesoporous-silica-nanoparticles-a-platform-for-drug-development
#8
Henrika Wickström, Ellen Hilgert, Johan O Nyman, Diti Desai, Didem Şen Karaman, Thomas de Beer, Niklas Sandler, Jessica M Rosenholm
Mesoporous silica nanoparticles (MSNs) have shown great potential in improving drug delivery of poorly water soluble (BCS class II, IV) and poorly permeable (BCS class III, IV) drugs, as well as facilitating successful delivery of unstable compounds. The nanoparticle technology would allow improved treatment by reducing adverse reactions of currently approved drugs and possibly reintroducing previously discarded compounds from the drug development pipeline. This study aims to highlight important aspects in mesoporous silica nanoparticle (MSN) ink formulation development for digital inkjet printing technology and to advice on choosing a method (2D/3D) for nanoparticle print deposit characterization...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29160732/optimization-and-characterization-of-sertaconazole-nitrate-flexisomes-embedded-in-hydrogel-for-improved-antifungal-activity
#9
Satish K Mandlik, Shridhar S Siras, Kiran R Birajdar
The aim of the present research work was to develop, characterize and optimize sertaconazole nitrate (STZN) embedded flexisomes (STZN-FS) to improve the cutaneous anti-fungal activity of STZN. Flexisomes are self-aggregating, flexible, deformable lipidic vesicles possessing an aqueous core. A 3(2) factorial design was implemented to optimize the effects of the critical material attributes of concentration of phospholipid (X1) and edge activator (X2) on the critical quality attributes of particle size (Y1), entrapment efficiency (Y2) and deformability index (Y3)...
November 21, 2017: Journal of Liposome Research
https://www.readbyqxmd.com/read/29160706/synthesis-and-characterization-of-ultralow-fouling-poly-n-acryloyl-glycinamide-brushes
#10
Fengyu Yang, Yonglan Liu, Yanxian Zhang, Baiping Ren, Jianxiong Xu, Jie Zheng
Rational design of biomaterials with antifouling properties still remains a challenge, but is important for many bench-to-bedside applications for biomedical implants, drug delivery carriers, and marine coatings. Herein we synthesized and characterized poly(N-acryloylglycinamide) (polyNAGA) and then grafted poly(NAGA) onto Au substrate to form polymer brushes with well controlled film stability, wettability and thickness using the surface-initiated atom transfer radical polymerization (SI-ATRP). The NAGA monomer integrates two hydrophilic amides on the side chain to enhance surface hydration, which is thought as a critical contributor to antifouling property...
November 21, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/29160624/buccal-patches-of-atenolol-formulated-using-fenugreek-trigonella-foenum-graecum-l-seed-mucilage
#11
Surya Narayan Ratha Adhikari, Satyabrata Panda
BACKGROUND: The use of mucoadhesive natural polymers in designing mucoadhesive patch systems has received much attention. OBJECTIVES: The study involved the development and evaluation of buccal patches of atenolol using fenugreek (Trigonella foenum-graecum L.) seed mucilage with hydroxylpropyl methyl cellulose (HPMC K4M) and a backing membrane (ethyl cellulose 5% w/v). MATERIAL AND METHODS: These atenolol-releasing buccal patches were prepared using a solvent casting technique...
January 2017: Polimery W Medycynie
https://www.readbyqxmd.com/read/29160601/metalated-chromene-and-chromone-complexes-ph-switchable-metal-carbon-bonding-interaction-photo-triggerable-chromone-delivery-application-and-antioxidative-activity
#12
Sze-Wing Ng, Lai-Hon Chung, Chi-Fung Yeung, Hoi-Shing Lo, Hau-Lam Shek, Tian-Shu Kang, Chung-Hang Leung, Chun-Yuen Wong
The two families of Ru(II)-chromene and -chromone complexes isolated in this work represent the first examples of metalated chromene and chromone complexes synthesized through transition-metal mediated cyclization of phenol-tethered ynone. These unprecedented metalated heterocyclic compounds exhibit remarkable features, such as pH-switchable metal-carbon bonding interactions, photo-triggerable release of organic chromone upon visible-light irradiation, and superior antioxidative property to their organic analog (1,4-benzopyrone)...
November 21, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/29160599/models-of-care-for-chronic-kidney-disease-a-systematic-review
#13
REVIEW
Ruairidh Nicoll, Lynn Robertson, Elliot Gemmell, Pawana Sharma, Corri Black, Angharad Marks
Chronic kidney disease (CKD) is common and presents an increasing burden to patients and health services. However, the optimal model of care for patients with CKD is unclear. We systematically reviewed the clinical effectiveness of different models of care for the management of CKD. A comprehensive search of eight databases was undertaken for articles published from 1992 to 2016. We included randomised controlled trials which assessed any model of care in the management of adults with pre-dialysis CKD, reporting renal, cardiovascular, mortality and other outcomes...
November 21, 2017: Nephrology
https://www.readbyqxmd.com/read/29160385/usual-interstitial-pneumonia-typical-possible-and-inconsistent-patterns
#14
Pedro Paulo Teixeira E Silva Torres, Marcelo Fouad Rabahi, Maria Auxiliadora Carmo Moreira, Gustavo de Souza Portes Meirelles, Edson Marchiori
Idiopathic pulmonary fibrosis is a severe and progressive chronic fibrosing interstitial lung disease, a definitive diagnosis being established by specific combinations of clinical, radiological, and pathological findings. According to current international guidelines, HRCT plays a key role in establishing a diagnosis of usual interstitial pneumonia (UIP). Current guidelines describe three UIP patterns based on HRCT findings: a typical UIP pattern; a pattern designated "possible UIP"; and a pattern designated "inconsistent with UIP", each pattern having important diagnostic implications...
September 2017: Jornal Brasileiro de Pneumologia: Publicaça̋o Oficial da Sociedade Brasileira de Pneumologia e Tisilogia
https://www.readbyqxmd.com/read/29160160/ideal-particle-sizes-for-inhaled-steroids-targeting-vocal-granulomas-preliminary-study-using-computational-fluid-dynamics
#15
Elizabeth L Perkins, Saikat Basu, Guilherme J M Garcia, Robert A Buckmire, Rupali N Shah, Julia S Kimbell
Objectives Vocal fold granulomas are benign lesions of the larynx commonly caused by gastroesophageal reflux, intubation, and phonotrauma. Current medical therapy includes inhaled corticosteroids to target inflammation that leads to granuloma formation. Particle sizes of commonly prescribed inhalers range over 1 to 4 µm. The study objective was to use computational fluid dynamics to investigate deposition patterns over a range of particle sizes of inhaled corticosteroids targeting the larynx and vocal fold granulomas...
November 1, 2017: Otolaryngology—Head and Neck Surgery
https://www.readbyqxmd.com/read/29160149/in-vitro-and-in-vivo-evaluation-of-silk-fibroin-functionalized-with-gaba-and-allopregnanolone-for-schwann-cell-and-neuron-survival
#16
Chiara Gm Gennari, Francesco Cilurzo, Nico Mitro, Donatella Caruso, Paola Minghetti, Valerio Magnaghi
AIM: This in vitro and in vivo study reports on silk fibroin (SF) scaffold, functionalized for in situ delivery of GABA and/or allopregnanolone (ALLO), as biomaterial for potential application in tissue engineering and nerve regeneration. MATERIALS & METHODS: We evaluated the feasibility to design 2D scaffolds (films) made of regenerated Bombyx mori SF, functionalized with GABA and/or ALLO to enhance in vitro biological functions, health, survival and growth of Schwann cells and sensitive neurons of the dorsal root ganglia...
November 21, 2017: Regenerative Medicine
https://www.readbyqxmd.com/read/29159921/pharmacokinetic-profile-of-ceftiofur-hydrochloride-injection-in-lactating-holstein-dairy-cows
#17
J Wang, H Peng, J Kong, T Zhao, S Zhang, X Cao
Ceftiofur (CEF), a broad-spectrum third-generation cephalosporin, exhibits a good activity against a broad range of gram-negative and gram-positive bacteria, including many that produce β-lactamase. To design a rational dosage regimen for the drug in lactating Holstein dairy cows, the pharmacokinetic properties of ceftiofur hydrochloride injection were investigated in six cows after intravenous, intramuscular, and subcutaneous administration of single dose of 2.2 mg/kg BW (body weight). Plasma concentration-time curves and relevant parameters were best described by noncompartmental analysis through WinNonlin 6...
November 21, 2017: Journal of Veterinary Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29159693/betahistine-dihydrochloride-transdermal-delivery-via-optimized-thermosensitive-gels-percutaneous-absorption-evaluation-using-rat-growth-as-a-biomarker
#18
Mohammed Hassan Elkomy, Shahira F El-Menshawe, Adel Ahmed Ali, Abdelkhalik Ali Halawa, Ahmed S G Srag El-Din
The aim of this study was to develop and optimize a betahistine dihydrochloride (BH) thermoreversible bioadhesive gel intended for transdermal delivery. The gels were obtained via cold method. A full factorial design was employed to investigate the joint effect of Poloxamer 407 concentration (18 and 20%), adhesive polymer type (Polyvinyl pyrolidone, Hydroxypropyl methylcellulose, and Carbopol 934), and adhesive polymer concentration (0.5 and 1.5%) on gelling temperature, viscosity at 37 °C, and adhesion strength...
November 20, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/29159346/peramivir-analogues-bearing-hydrophilic-side-chains-exhibit-higher-activities-against-h275y-mutant-than-wild-type-influenza-virus
#19
Din-Chi Chiu, Tzu-Chen Lin, Wen-I Huang, Ting-Jen Cheng, Keng-Chang Tsai, Jim-Min Fang
Peramivir is an effective anti-influenza drug in the clinical treatment of influenza, but its efficacy toward the H275Y mutant is reduced. The previously reported cocrystal structures of inhibitors in the mutant neuraminidase (NA) suggest that the hydrophobic side chain should be at the origin of reduced binding affinity. In contrast, zanamivir having a hydrophilic glycerol side chain still possesses high affinity toward the H275Y NA. We thus designed five peramivir analogues (5-9) carrying hydrophilic glycol or glycerol side chains, and evaluated their roles in anti-influenza activity, especially for the H275Y mutant...
November 21, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/29159213/dataset-generated-for-dissection-of-mechanisms-of-trypanothione-reductase-and-tryparedoxin-peroxidase-through-dynamic-network-analysis-and-simulations-in-leishmaniasis
#20
Anurag Kumar, Bhaskar Saha, Shailza Singh
Leishmaniasis is the second largest parasitic killer disease caused by the protozoan parasite Leishmania, transmitted by the bite of sand flies. It's endemic in the eastern India with 165.4 million populations at risk with the current drug regimen. Three forms of leishmaniasis exist in which cutaneous is the most common form caused by Leishmania major. Trypanothione Reductase (TryR), a flavoprotein oxidoreductase, unique to thiol redox system, is considered as a potential target for chemotherapy for trypanosomatids infection...
December 2017: Data in Brief
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