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https://www.readbyqxmd.com/read/28813027/sulfonamide-linked-ciprofloxacin-sulfadiazine-and-amantadine-derivatives-as-a-novel-class-of-inhibitors-of-jack-bean-urease-synthesis-kinetic-mechanism-and-molecular-docking
#1
Pervaiz Ali Channar, Aamer Saeed, Fernando Albericio, Fayaz Ali Larik, Qamar Abbas, Mubashir Hassan, Hussain Raza, Sung-Yum Seo
Sulfonamide derivatives serve as an important building blocks in the drug design discovery and development (4D) process. Ciprofloxacin-, sulfadiazine- and amantadine-based sulfonamides were synthesized as potent inhibitors of jack bean urease and free radical scavengers. Molecular diversity was explored and electronic factors were also examined. All 24 synthesized compounds exhibited excellent potential against urease enzyme. Compound 3e (IC50 = 0.081 ± 0.003 µM), 6a (IC50 = 0.0022 ± 0.0002 µM), 9e (IC50 = 0...
August 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28812999/synthesis-and-evaluation-of-a-sodium-alginate-4-aminosalicylic-acid-based-microporous-hydrogel-for-potential-viscosupplementation-for-joint-injuries-and-arthritis-induced-conditions
#2
Dharmesh R Chejara, Mostafa Mabrouk, Pradeep Kumar, Yahya E Choonara, Pierre P D Kondiah, Ravindra V Badhe, Lisa C du Toit, Divya Bijukumar, Viness Pillay
A microporous hydrogel was developed using sodium alginate (alg) and 4-aminosalicylic acid (4-ASA). The synthesized hydrogel was characterized using various analytical techniques such as Fourier transform infrared spectroscopy (FTIR), Carbon-13 nuclear magnetic resonance ((13)C-NMR), X-ray powder diffraction (XRD), scanning electron microscopy (SEM), and differential scanning calorimetry (DSC). Additonal carboxyl and hydroxyl functional groups of 4-ASA provided significant lubrication and stress-triggered sol-gel transition to the conjugated hydrogel...
August 16, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28812983/a-microfluidic-platform-for-modeling-metastatic-cancer-cell-matrix-invasion
#3
Laura Blaha, Chentian Zhang, Mario Cabodi, Joyce Y Wong
Invasion of the extracellular matrix is a critical step in the colonization of metastatic tumors. The invasion process is thought to be driven by both chemokine signaling and interactions between invading cancer cells and physical components of the metastatic niche, including endothelial cells that line capillary walls and serve as a barrier to both diffusion and invasion of the underlying tissue. Transwell chambers, a tool for generating artificial chemokine gradients to induce cell migration, have facilitated recent work to investigate the chemokine contributions to matrix invasion...
August 16, 2017: Biofabrication
https://www.readbyqxmd.com/read/28812379/dietary-polyphenols-for-atherosclerosis-a-comprehensive-review-and-future-perspectives
#4
Roodabeh Bahramsoltani, Farnaz Ebrahimi, Mohammad Hosein Farzaei, Armaghan Baratpourmoghaddam, Pardis Ahmadi Borkani, Pourouchista Rostamiasrabadi, Amir Hosein Rasouli Amirabadi, Roja Rahimi
Atherosclerosis is one of the most prevalent reasons for premature death in adults. Despite the several conventional drugs in the market; many patients are not completely treated. Here we comprehensively review current clinical evidence regarding the efficacy of dietary polyphenols in atherosclerosis and related complications. PubMed, Cochrane library and Scopus were searched from inception until August 2016 to obtain clinical trials in which polyphenols were evaluated in cardiovascular parameters related to atherosclerosis...
August 16, 2017: Critical Reviews in Food Science and Nutrition
https://www.readbyqxmd.com/read/28812361/ultrasensitive-and-accurate-assay-of-human-methyltransferase-activity-at-the-single-cell-level-based-on-a-single-integrated-magnetic-microprobe
#5
Haiyan Zhao, Lei Wang, Weiqi Li, Shumei Zhai, Wei Jiang
Human DNA methyltransferase (MTase) activity expression patterns and inhibition response are linked to related cancer initiation, progression and therapeutic responses. Sensitive and accurate human MTase activity assay in cancer cells, especially at the single-cell level, is essential for biological study, clinical diagnosis and therapy. Here, we developed an ultrasensitive and accurate DNA (cytosine-5)-methyltransferase 1 (Dnmt1) activity assay at the single-cell level based on a single integrated magnetic microprobe of functionalized double-stranded DNA (dsDNA) anchored to a single magnetic microbead surface...
August 16, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28812358/bioinspired-active-stealth-magneto-nanomicelles-for-theranostics-combining-efficient-mri-and-enhanced-drug-delivery
#6
Kai-Long Zhang, Jie Zhou, Hong Zhou, Ying Wu, Rui Liu, Li-Li Wang, Wei-Wen Lin, Guoming Huang, Huang-Hao Yang
The mononuclear phagocyte system (MPS), with key roles in recognition and clearance of foreign particles, is a major constraint to nanoparticle-based delivery systems. The desire to improve the delivery efficiency has prompted the search for stealthy long-circulating nanoplatforms. Herein, we design an antiphagocytic delivery system with "active" stealth behavior for cancer theranostics combining efficient MRI and enhanced drug delivery. We modify self-peptide, a synthetic peptide for active immunomodulation, to biodegradable poly (lactide-glycolide)-poly (ethylene glycol) (PLGA-PEG), then utilize the self-assembly properties of PLGA-PEG to form nanomicelles that encapsulating iron oxide (IO) nanoparticles and anticancer drug paclitaxel (PTX)...
August 16, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28812347/rational-design-of-polymeric-nanoparticles-with-tailorable-biomedical-functions-for-cancer-therapy
#7
Wenhai Lin, Wei Zhang, Tingting Sun, Shi Liu, Yu Zhu, Zhigang Xie
Polymeric nanoparticles (NPs) play a key role in nanoscale formulations for bioimaging, cancer treatment and theranostics. In this work, we designed and synthesized a series of hydrophobic polymers (P1-6) with different pendent groups via one-step multicomponent Passerini reaction. These polymers possessed similar molecular structures and various biomedical functions. Interestingly, they could self-assemble into stable NPs in aqueous media. All formed NPs were redox-sensitive because of the existence of disulfide bonds in the backbone...
August 16, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28812327/design-and-synthesis-of-terephthalic-acid-based-histone-deacetylase-inhibitors-with-dual-stage-anti-plasmodium-activity
#8
Katharina Stenzel, Ming Jang Chua, Sandra Duffy, Yevgeniya Antonova-Koch, Stephan Meister, Alexandra Hamacher, Matthias U Kassack, Elizabeth A Winzeler, Vicky M Avery, Thomas Kurz, Katherine T Andrews, Finn Kristian Hansen
In this work we aimed to develop parasite-selective HDAC inhibitors with activity against the disease-causing asexual blood stages of Plasmodium as well as causal prophylactic and/or transmission blocking properties. We report the design, synthesis and biological testing of a series of 13 terephthalic acid-based histone deacetylase inhibitors. All compounds showed low cytotoxicity against human embryonic kidney (HEK293) cells (IC50 8 - >51 µM), with 11 also having sub-micromolar in vitro activity against drug-sensitive (3D7) and multi-drug resistant (Dd2) asexual blood stage Plasmodium falciparum parasites (IC50 ~ 0...
August 15, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28812281/preclinical-development-of-an-automated-injection-device-for-intradermal-delivery-of-a-cell-based-therapy
#9
Giulia Leoni, Alex Lyness, Patrick Ginty, Rindi Schutte, Gopalan Pillai, Gayatri Sharma, Paul Kemp, Natalie Mount, Michaela Sharpe
Current methods for intradermal delivery of therapeutic products in clinical use include manual injection via the Mantoux technique and the use of injection devices, primarily developed for the delivery of vaccines and small molecules. A novel automated injection device is presented specifically designed for accurate delivery of multiple doses of product through a number of adjustable injection parameters, including injection depth, dose volume and needle insertion speed. The device was originally conceived for the delivery of a cell-based therapy to patients with skin wounds caused by epidermolysis bullosa...
August 15, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28812225/enhancement-of-ocular-efficacy-of-aceclofenac-using-biodegradable-plga-nanoparticles-formulation-and-characterization
#10
Rajesh Katara, Sameer Sachdeva, Dipak K Majumdar
In the present study, an effort was made to design poly (D, L-lactide-co-glycolide) acid nanoparticles of aceclofenac by direct precipitation method. The nanoparticles were found to have adequate particle size range for ocular administration of 162.6 to 244.13 nm with nearly spherical shape and with zeta potential of - 21.5 to - 25.5 mV. Drug entrapment efficiency of nanoparticle formulations ranged from 42.9 to 92.68%. Differential scanning calorimetric (DSC) and powder X-ray diffraction (PXRD) studies depicted that the drug incorporated in nanoparticles was found to be in amorphous state...
August 15, 2017: Drug Delivery and Translational Research
https://www.readbyqxmd.com/read/28812060/reolysin-and-histone-deacetylase-inhibition-in-the-treatment-of-head-and-neck-squamous-cell-carcinoma
#11
Alena C Jaime-Ramirez, Jun-Ge Yu, Enrico Caserta, Ji Young Yoo, Jianying Zhang, Tae Jin Lee, Craig Hofmeister, John H Lee, Bhavna Kumar, Quintin Pan, Pawan Kumar, Robert Baiocchi, Theodoros Teknos, Flavia Pichiorri, Balveen Kaur, Matthew Old
Oncolytic viruses (OVs) are emerging as powerful anti-cancer agents and are currently being tested for their safety and efficacy in patients. Reovirus (Reolysin), a naturally occurring non-pathogenic, double-stranded RNA virus, has natural oncolytic activity and is being tested in phase I-III clinical trials in a variety of tumor types. With its recent US Food and Drug Administration (FDA) orphan drug designation for several tumor types, Reolysin is a potential therapeutic agent for various cancers, including head and neck squamous cell carcinomas (HNSCCs), which have a 5-year survival of ∼55%...
June 16, 2017: Molecular Therapy Oncolytics
https://www.readbyqxmd.com/read/28812044/monte-carlo-simulations-of-randomized-clinical-trials-in-epilepsy
#12
Daniel M Goldenholz, Joseph Tharayil, Robert Moss, Evan Myers, William H Theodore
BACKGROUND: The placebo response in epilepsy randomized clinical trials (RCTs) has recently been shown to largely reflect underlying natural variability in seizure frequency. Based on this observation, we sought to explore the parameter space of RCT design to optimize trial efficiency and cost. METHODS: We used one of the world's largest patient reported seizure diary databases, SeizureTracker.com to derive virtual patients for simulated RCTs. We ran 1000 randomly generated simulated trials using bootstrapping (sampling with replacement) for each unique combination of trial parameters, sweeping a large set of parameters in durations of the baseline and test periods, number of patients, eligibility criteria, drug effect size, and patient dropout...
August 2017: Annals of Clinical and Translational Neurology
https://www.readbyqxmd.com/read/28811833/nsitematch-prediction-of-binding-sites-of-nucleotides-by-identifying-the-structure-similarity-of-local-surface-patches
#13
Jie Sun, Ke Chen
Nucleotides play a central role in life-form metabolism, by interacting with proteins and mediating the function of proteins. It is estimated that nucleotides constitute about 15% of the biologically relevant ligands included in PDB. Prediction of binding sites of nucleotides is useful in understanding the function of proteins and can facilitate the in silico design of drugs. In this study, we propose a nucleotide-binding site predictor, namely, NSiteMatch. The NSiteMatch algorithm integrates three different strategies: geometrical analysis, energy calculation, and template comparison...
2017: Computational and Mathematical Methods in Medicine
https://www.readbyqxmd.com/read/28811659/identification-synthesis-and-biological-activity-of-alkyl-guanidine-oligomers-as-potent-antibacterial-agents
#14
C Zamperini, G Maccari, D Deodato, C Pasero, I D'Agostino, F Orofino, F De Luca, E Dreassi, J D Docquier, M Botta
In the last two decades, the repertoire of clinically effective antibacterials is shrinking due to the rapidly increasing of multi-drug-resistant pathogenic bacteria. New chemical classes with innovative mode of action are required to prevent a return to the pre-antibiotic era. We have recently reported the identification of a series of linear guanidine derivatives and their antibacterial properties. A batch of a promising candidate for optimization studies (compound 1) turned out to be a mixture containing two unknown species with a better biological activity than the pure compound...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811600/exploring-leishmania-secretory-proteins-to-design-b-and-t-cell-multi-epitope-subunit-vaccine-using-immunoinformatics-approach
#15
Nazia Khatoon, Rajan Kumar Pandey, Vijay Kumar Prajapati
Visceral leishmaniasis (VL) is a fatal form of leishmaniasis which affects 70 countries, worldwide. Increasing drug resistance, HIV co-infection, and poor health system require operative vaccination strategy to control the VL transmission dynamics. Therefore, a holistic approach is needed to generate T and B memory cells to mediate long-term immunity against VL infection. Consequently, immunoinformatics approach was applied to design Leishmania secretory protein based multi-epitope subunit vaccine construct consisting of B and T cell epitopes...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811524/synthesis-of-sulfo-sialic-acid-analogues-potent-neuraminidase-inhibitors-in-regards-to-anomeric-functionality
#16
Christopher J Vavricka, Chiaki Muto, Tomohisa Hasunuma, Yoshinobu Kimura, Michihiro Araki, Yan Wu, George F Gao, Hiroshi Ohrui, Minoru Izumi, Hiromasa Kiyota
The design, synthesis and application of N-acetylneuraminic acid-derived compounds bearing anomeric sulfo functional groups are described. These novel compounds, which we refer to as sulfo-sialic acid analogues, include 2-decarboxy-2-deoxy-2-sulfo-N-acetylneuraminic acid and its 4-deoxy-3,4-dehydrogenated pseudoglycal. While 2-decarboxy-2-deoxy-2-sulfo-N-acetylneuraminic acid contains no further modifications of the 2-deoxy-pyranose ring, it is still a more potent inhibitor of avian-origin H5N1 neuraminidase (NA) and drug-resistant His275Tyr NA as compared to the oxocarbenium ion transition state analogue 2,3-dehydro-2-deoxy-N-acetylneuraminic acid...
August 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28811131/assessment-of-translational-risk-in-drug-research-role-of-biomarker-classification-and-mechanism-based-pkpd-concepts
#17
Sandra A G Visser, Tjerk J H Bueters
In 2005, Danhof and coauthors proposed a new biomarker classification in the context of the application of mechanism-based PKPD modeling. They defined the term 'biomarker' as a measure that characterizes a drug-induced response, which is on the causal path between drug administration and clinical outcome. The biomarker classification identified seven categories that provide different insights into the kinetics of drug action, such as target site distribution, target engagement, or into the impact of the drug on physiology or disease...
August 12, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28811102/high-resolution-separations-of-charge-variants-and-disulfide-isomers-of-monoclonal-antibodies-and-antibody-drug-conjugates-using-ultra-high-voltage-capillary-electrophoresis-with-high-electric-field-strength
#18
W Hampton Henley, Yan He, J Scott Mellors, Nicholas G Batz, J Michael Ramsey, James W Jorgenson
Ultra-high voltage capillary electrophoresis with high electric field strength has been applied to the separation of the charge variants, drug conjugates, and disulfide isomers of monoclonal antibodies. Samples composed of many closely related species are difficult to resolve and quantify using traditional analytical instrumentation. High performance instrumentation can often save considerable time and effort otherwise spent on extensive method development. Ideally, the resolution obtained for a given CE buffer system scales with the square root of the applied voltage...
July 29, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28810949/analysis-of-non-pivotal-bioequivalence-studies-submitted-in-abbreviated-new-drug-submissions-for-delayed-release-drug-products
#19
Paramjeet Kaur, Xiaojian Jiang, Ethan Stier
The US FDA's rule on "Requirements for Submission of Bioequivalence Data" requiring submission of all bioequivalence (BE) studies conducted on the same formulation of the drug product submitted for approval was published in Federal Register in January 2009. With the publication of this rule, we evaluated the impact of data from non-pivotal BE studies in assessing BE and identified the reasons for failed in vivo BE studies for generic oral delayed-release (DR) drug products only. We searched the Agency databases from January 2009 toDecember 2016 to identify Abbreviated New Drug Applications (ANDAs) submitted for DR drug products containing non-pivotal BE studies...
2017: Journal of Pharmacy & Pharmaceutical Sciences: a Publication of the Canadian Society for Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28810188/novel-tacrine-derivatives-exhibiting-improved-acetylcholinesterase-inhibition-design-synthesis-and-biological-evaluation
#20
Eeda Koti Reddy, Chandran Remya, Kumar Mantosh, Ayyiliath M Sajith, R V Omkumar, C Sadasivan, Shaik Anwar
A novel series of twenty four tacrine derivatives were designed and synthesised. Among these, thirteen were taken for the acetylcholinesterase (AChE) inhibition studies. Three compounds such as 4c, 6c and 6f were found to possess significant AChE inhibitory properties with IC50 values 12.97 ± 0.47 nM, 5.17 ± 0.24 nM and 7.14 ± 0.78 nM respectively. In silico docking studies revealed that these compounds can bind strongly in the active site of the enzyme and prevent enzyme-substrate interactions...
August 5, 2017: European Journal of Medicinal Chemistry
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