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Drug Research

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https://www.readbyqxmd.com/read/28222467/design-and-synthesis-of-new-1-3-4-oxadiazole-benzothiazole-and-hydrazone-derivatives-as-promising-chemotherapeutic-agents
#1
Betül Kaya, Weiam Hussin, Leyla Yurttaş, Gülhan Turan-Zitouni, Hülya Karaca Gençer, Merve Baysal, Abdullah Burak Karaduman, Zafer Asim Kaplancıklı
Looking for new cytotoxic and antimicrobial agents with improved antitumor activity, a series of hydrazide and oxadiazole derivatives were designed and synthesized using 3-methoxyphenol as starting substance. Novel N'-(arylidene)-2-(3-methoxyphenoxy)acetohydrazide derivatives (4a-f)/1-(4-substitutedphenyl)-2-[(5-[(3-methoxyphenoxy)methyl]-1,3,4-oxadiazol-2-yl)thio]ethan-1-one derivatives (6a-f)/N-(6-substitutedbenzothiazol-2-yl)-2-[(5-[(3-methoxyphenoxy)methyl]-1,3,4-oxadiazol-2-yl)thio]acetamide derivatives (7a-e) were obtained and evaluated for their in vitro antimicrobial activity against various gram-positive, gram-negative bacteria and fungi...
February 21, 2017: Drug Research
https://www.readbyqxmd.com/read/28222466/cromolyn-sodium-attenuates-paraquat-induced-lung-injury-by-modulation-of-proinflammatory-cytokines
#2
Amir Larki Harchegani, Ali Asghar Hemmati, Amir Nili-Ahmadabadi, Borhan Darabi, Somayeh Shabib
The current study aimed to investigate the effects of Cromolyn Sodium (CS) on proinflammatory cytokines in Paraquat (PQ)-induced lung damage in rat. Animals were randomly divided into 5 groups. Group 1 and 2 received nebulized vehicle and CS (8 mg/kg) for 3 consecutive weeks, respectively. Group 3 was treated with single oral dose of PQ (40 mg/kg). Groups 4 and 5 were PQ groups which received nebulized CS (6 and 8 mg/kg/day, respectively) from 1 week before to 2 weeks after PQ administration. Finally, the animals were scarified and the changes of hydroxyproline (HP) and histology were evaluated in lung tissue...
February 21, 2017: Drug Research
https://www.readbyqxmd.com/read/28212595/preparation-and-characterization-of-gold-nanoparticles-in-the-presence-of-citrate-and-soybean-seed-extract-in-an-acidic-conditions
#3
Ebrahim Izadi, Ali Rasooli, Abolfazl Akbarzadeh, Soodabeh Davaran
Through the present study, an eco-friendly method was used to synthesize the gold nanoparticles (GNPs) by using the sodium citrate and extract of the soybean seed as reducing the agents at PH 3. X-Ray diffraction (XRD) method was used to evaluate the crystal structure of as-synthesized NPs and it's revealed that this method leads to well crystallized GNPs. In order to determine the particle size and their distribution, field emission scanning microscopy (FE-SEM) and dynamic light scattering (DLS) were used...
February 17, 2017: Drug Research
https://www.readbyqxmd.com/read/28208189/advances-in-silver-nanotechnology-an-update-on-biomedical-applications-and-future-perspectives
#4
Shiva Gholizadeh-Ghaleh Aziz, Sara Gholizadeh-Ghaleh Aziz, Abolfazl Akbarzadeh
Nanotechnology is one of the most promising fields for producing new applications in nanotechnology, biotechnology, and medicine. However, only a few products have been used for nanotechnology, biotechnology, and medical purposes. Nanoparticles have been among the most usually applied nanomaterial in our health care system for hundreds of years. The most prominent nano product is nano silver which generally present at 1-100 nm in size in at least one dimension. Silver nanoparticles reveal remarkably unusual chemical, physical and biological properties and have been used for many different applications which detailed in this review...
February 16, 2017: Drug Research
https://www.readbyqxmd.com/read/28196394/synthesis-and-evaluation-of-a-triblock-copolymer-zno-nanoparticles-from-poly-%C3%AE%C2%B5-caprolactone-and-poly-acrylic-acid-as-a-potential-drug-delivery-carrier
#5
Lida Ahmadkhani, Ali Baghban, Shahram Mohammadpoor, Rovshan Khalilov, Abolfazl Akbarzadeh, Taras Kavetskyy, Siamak Saghfi, Aygun N Nasibova
Through the present paper, a triblock copolymer containing pH-responsive (polyacrylic acid-b-polycaprolactone -b-polyacrylic acid) (PAA-b-PCL-b-PAA) was synthesized by using the ring-opening polymerization (ROP) of ε-caprolactone (ε-CL) and the reversible addition fragmentation chain transfer (RAFT) polymerization of the acrylic acid methods, as the drug carrier. Blends of the nanocrystalline zinc oxide nanoparticles (n-ZnO) and triblock copolymer treated from the solution have been used to make the hybrid polymer-metal oxide for the preparation of the drug loaded nanocomposite...
February 14, 2017: Drug Research
https://www.readbyqxmd.com/read/28166590/the-effect-of-chrysin-loaded-plga-peg-on-metalloproteinase-gene-expression-in-mouse-4t1-tumor-model
#6
Zoheyr Mohammadi, Mohsen Sharif Zak, Khaled Seidi, Meisam Barati, Abolfazl Akbarzadeh, Nosratollah Zarghami
Despite the advances in medicine, cancer remains as one of the leading causes of the death worldwide. Through our previous study, the Chrysin loaded PGLA/PEG has been synthesized, and its physico-chemical properties were characterized. The aim of the present study was to evaluate the Chrysin loaded PGLA/PEG nanoparticle therapeutic effects on TIMP-1, TIMP-2, MMP-2, MMP-9 and PI3k expression in Mouse 4T1 breast tumor model.30 mice were enrolled in the current study, and the mice were randomly divided into 3 groups: untreated (n=10), Chrysin treatment (n=10) and Chrysin-loaded PLGA/PEG-based treatment (n=10)...
February 6, 2017: Drug Research
https://www.readbyqxmd.com/read/28158894/is-the-inhibition-of-dipeptidyl-peptidase-4-ddp-4-enzyme-route-dependent-and-or-driven-by-high-peak-concentration-seeking-answers-with-zydpla1-a-novel-long-acting-dpp-4-inhibitor-in-a-rodent-model
#7
Harilal Patel, Amit A Joharapurkar, Rajesh Bahekar, Prakash Patel, Samadhan G Kshirsagar, Nirav Modi, Ashok Ghoghari, Vishal J Patel, Mukul R Jain, Nuggehally R Srinivas, Pankaj R Patel, Ranjit C Desai
ZYDPLA1 is a long acting enzyme dipeptidyl peptidase-4 (DPP-4) inhibitor. The comparative effect of DPP-4 inhibition after intravenous (IV) and oral administration of ZYDPLA1 in a rat model was evaluated to answer the question of route dependency and/or the need of high plasma levels of ZYDPLA1. The study was conducted using parallel design in male Wistar rats for IV/oral route (n=9 and 6, for IV and oral respectively). A single 30 mg/kg dose of ZYDPLA1 was administered. Plasma samples were analysed for ZYDPLA1 concentration and DPP-4 inhibition...
February 3, 2017: Drug Research
https://www.readbyqxmd.com/read/28158893/efficacy-and-safety-of-phytosomal-curcumin-in-non-alcoholic-fatty-liver-disease-a-randomized-controlled-trial
#8
Yunes Panahi, Parisa Kianpour, Reza Mohtashami, Ramezan Jafari, Luis E Simental-Mendía, Amirhossein Sahebkar
Non-alcoholic fatty liver disease (NAFLD) is a common liver disease characterized by excess lipid deposition in the hepatic tissue and subsequent oxidative and inflammatory damage. Curcumin is a dietary polyphenol with lipid-modifying, antioxidant and anti-inflammatory properties. This study aimed to evaluate the efficacy and safety of supplementation with phytosomal curcumin in subjects with NAFLD.Patients diagnosed with NAFLD (grades 1-3 according to liver ultrasonography) were randomly assigned to the curcumin (phytosomal form; 1 000 mg/day in 2 divided doses) (n=50) or placebo group (n=52) for a period of 8 weeks...
February 3, 2017: Drug Research
https://www.readbyqxmd.com/read/28158892/immunomodulatory-study-of-different-solvent-extract-of-elephantopus-scaber-linn
#9
Sachin M Hiradeve, Vinod D Rangari
The aim and objective of present study is that to provide a scientific evidence for the immunomodulatory potential of Elephantopus scaber in vivo. The immunomodulatory activity was performed in petroleum ether, solvent ether, methanol and aqueous extract of aerial part and root of E. scaber by using models such as delayed type hypersensitivity, humoral antibody response to SRBC and carbon clearance test for phagocytic activity in Wistar rat. The observation and results of present study suggested that among the total 8 extract, only the petroleum ether and solvent ether aerial part extract of E...
February 3, 2017: Drug Research
https://www.readbyqxmd.com/read/28142160/influence-of-tiopronin-on-the-metabolism-of-alcohol-in-healthy-subjects
#10
Friederike Nass, Berthold Schneider, Stefan Wilm, Bernd Kardel, Elisabeth Gabor, Fabian Merges, Michael Kroll
Drug safety- and drug-alcohol interaction studies have mainly been conducted for frequently prescribed drugs with high financial interests. Orphan drugs such as tiopronin (ORPHA25073) are often neglected in terms of clinical research. Tiopronin is a drug that is mainly used for the treatment of cystinuria. In this study, the interaction of tiopronin regarding the metabolism of alcohol (primary objective), and the safety of tiopronin in combination with alcohol was tested in healthy volunteers.In this randomised, double-blind, cross-over study, 13 healthy subjects received 500 mg tiopronin or an identical looking placebo 1 h before the intake of 0...
January 31, 2017: Drug Research
https://www.readbyqxmd.com/read/28118672/antidiabetic-activity-of-extract-and-compounds-from-an-endophytic-fungus-nigrospora-oryzae
#11
Philip F Uzor, Patience O Osadebe, Ngozi J Nwodo
The fungal extract as well as the 3 biosynthetic compounds, (S)-(+)-2-cis-4-trans-abscisic acid (1), , 7'-hydroxy-abscisic acid (2) and 4-des-hydroxyl altersolanol A (3) from the endophytic fungus, Nigrospora oryzae, isolated from Combretum dolichopetalum leaf were investigated for their antidiabetic potential.The antidiabetic activity was determined in alloxan-induced diabetic mice by monitoring their fasting blood sugar for 9 h.The extract and the compounds (1-3) significantly (p<0.001) reduced the fasting blood sugar of the diabetic mice...
January 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28118671/mechanistic-approach-for-toxic-effects-of-bupropion-in-primary-rat-hepatocytes
#12
Elham Ahmadian, Hossein Babaei, Alireza Mohajjel Nayebi, Aziz Eftekhari, Mohammad Ali Eghbal
Bupropion is a widely prescribed antidepressant/smoke cessation drug. However, hepatotoxicity is one of its side effects reported in some recipients. The mechanisms by which bupropion induces hepatotoxicity is not clear yet. This experiment was intended to assess the cytotoxic mechanisms of bupropion toward primary rat hepatocytes. Additionally, the effect of α-tocopherol succinate (ALPHA-TOS) and N-acetyl cysteine (NAC) and mitochondrial permeability transition (MPT) pore sealing agent cyclosporine A (Cs A) on this toxicity was investigated...
January 24, 2017: Drug Research
https://www.readbyqxmd.com/read/28076878/sumatriptan-an-antimigraine-drug-inhibits-pentylenetetrazol-induced-seizures-in-nmri-mice
#13
Abolfazl Jand, Mohammad Palizvan
Sumatriptan has been used for the acute treatment of migraine attacks. There are many similarities between migraine and epilepsy and the medications used to treat one of these disorders can effectively be used to treat the other. The purpose of this study was to evaluate and compare the anticonvulsant effects of sumatriptan with sodium valproate in NMRI mice. 62 male NMRI mice were divided into 8 groups. The groups consisted of a saline (control) group, 4 intraperitoneally (ip) administered sumatriptan groups (1, 10, 50, and 100 mg/kg, ip), and 3 sodium valproate groups (50, 150, and 300 mg/kg, ip)...
January 11, 2017: Drug Research
https://www.readbyqxmd.com/read/28073115/pyridazine-based-scaffolds-as-privileged-structures-in-anti-cancer-therapy
#14
M Jaballah, R Serya, K Abouzid
Pyridazines, their oxo derivatives; pyridazinone as well as fused bi- or tricyclic pyridazine containing scaffolds are key structural features of many biologically active compounds with diverse pharmacological applications, including cancer therapy. Since protein kinases play prominent role in tumor biology, the inhibition of its signaling pathway is considered an effective therapeutic option for the treatment of cancer.Based on the various advantages of pyridazines in drug design including modulation of the physico-chemical properties, improving ADME and toxicity profile as well as easy and diverse synthetic methods of access, makes them an invaluable tool for designing compounds as future drugs for targeted cancer treatment...
January 10, 2017: Drug Research
https://www.readbyqxmd.com/read/28073114/a-study-of-acute-poisoning-cases-admitted-to-the-university-hospital-emergency-department-in-tabriz-iran
#15
Mehdi Oraie, Mir-Jamal Hosseini, Mina Islambulchilar, Seyed-Hasan Hosseini, Mehdi Ahadi-Barzoki, Habib Sadr, Hashem Yaghoubi
Chemical substances have an important threat due to extensive use in medicine, agriculture, industry and environment. In this retrospective study, etiological and demographic characteristics of acute poisoning cases admitted to a hospital in Iran were investigated. We compared these data with those reported from other parts of the country and the international experiences to evaluate any difference if exists. 7 052 poisoned cases admitted to the hospital from April 2006 to March 2013, by data collected from the medical record in poison center section...
January 10, 2017: Drug Research
https://www.readbyqxmd.com/read/27992936/role-of-isradipine-loaded-solid-lipid-nanoparticles-on-the-pharmacodynamic-effect-in-rats
#16
G Thirupathi, E Swetha, D Narendar
Isradipine (ID), is an antihypertensive drug, having low oral bioavailability (15-24%) due to poor aqueous solubility (0.01 mg/mL) and also hepatic first-pass metabolism. Among various approaches, Solid lipid nanoparticles (SLNs) were developed using stearic acid, glyceryl monostearate as lipid matrices for improving the oral bioavailability of ID. ID-SLNs were prepared by using hot homogenization followed by ultrasonication. The prepared SLNs were characterized for size, PDI, zeta potential (ZP), entrapment efficiency (EE) and drug content...
December 19, 2016: Drug Research
https://www.readbyqxmd.com/read/27992935/qsar-differential-model-for-prediction-of-sirt1-modulation-using-monte-carlo-method
#17
A Kumar, S Chauhan
Silent information regulator 2 homologue one (SIRT1) modulators have therapeutic potential for a number of diseases like cardiovascular, metabolic, inflammatory and age related disorders. Here, we have studied both activators and inhibitors of SIRT1 and constructed differential quantitative structure activity relationship (QSAR) models using CORAL software by Monte Carlo optimization method and SMILES notation. 3 splits divided into 3 subsets: sub-training, calibration and test sets, were examined and validated with a prediction set...
December 19, 2016: Drug Research
https://www.readbyqxmd.com/read/27992934/novel-99mtc-radiolabeled-anionic-linear-globular-peg-based-dendrimer-chlorambucil-non-invasive-method-for-in-vivo-biodistribution
#18
S M Ghoreishi, A Khalaj, A B-Rajabi, A D Azar, M S Ardestani, A Assadi
Chlorambucil (CBL) is an alkylating agent, which widely use in the treatment of various types of tumors. The main purpose of this study is to evaluate the in-vivo biodistribution of CBL conjugated to the anionic dendrimer, which has a great ability to labeled with (99m)Tc through binding to carboxylate terminate groups. Whole body scans were used to analyze the percentage of the injected dose in different times. Radiochemical purity (RCP) and in-vivo biodistribution were also calculated with the SPECT/CT instrument...
December 19, 2016: Drug Research
https://www.readbyqxmd.com/read/27926950/c6-and-c7-substituted-3-4-dihydro-2-1h-quinolinones-as-inhibitors-of-monoamine-oxidase
#19
L Meiring, J Petzer, A Petzer
Purpose Monoamine oxidase (MAO) inhibitors are considered to be useful therapeutic agents and isoform specific inhibitors are employed for the treatment of depression and Parkinson's disease. MAO inhibitors are also under investigation for the treatment of disorders ranging from Alzheimer's disease, prostate cancer and certain cardiomyopathies. While a number of irreversible MAO inhibitors are available in the clinic, reversible inhibitors, particularly of the MAO-B isoform are still being developed. Based on our interest in discovering reversible inhibitors with specificity for MAO-B, we have recently reported that, among a series of 10 3,4-dihydro-2(1H)-quinolinone derivatives, are high potency MAO-B inhibitors, with a number of homologues displaying good selectivities for MAO-B over the MAO-A isoform...
December 7, 2016: Drug Research
https://www.readbyqxmd.com/read/27926949/efficacy-and-tolerability-of-co-administering-full-%C3%A2%C2%B5-opioid-receptor-agonists-with-buprenorphine-and-mixed-opioid-agonists
#20
X Ruan, J Luo, A Kaye
No abstract text is available yet for this article.
December 7, 2016: Drug Research
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