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https://www.readbyqxmd.com/read/29031078/structural-design-synthesis-and-pharmacological-evaluation-of-thiazoles-against-trypanosoma-cruzi
#1
Gevanio Bezerra de Oliveira Filho, Marcos Veríssimo de Oliveira Cardoso, José Wanderlan Pontes Espíndola, Dayane Albuquerque Oliveira E Silva, Rafaela Salgado Ferreira, Pollyanne Lacerda Coelho, Pâmela Silva Dos Anjos, Emanuelle de Souza Santos, Cássio Santana Meira, Diogo Rodrigo Magalhaes Moreira, Milena Botelho Pereira Soares, Ana Cristina Lima Leite
Chagas disease is one of the most significant health problems in the American continent. benznidazole (BDZ) and nifurtimox (NFX) are the only drugs approved for treatment and exhibit strong side effects and ineffectiveness in the chronic stage, besides different susceptibility among T. cruzi DTUs (Discrete Typing Units). Therefore, new drugs to treat this disease are necessary. Thiazole compounds have been described as potent trypanocidal agents. Here we report the structural planning, synthesis and anti-T...
September 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031072/recent-advances-in-discovery-and-development-of-natural-products-as%C3%A2-source-for-anti-parkinson-s-disease-lead-compounds
#2
REVIEW
Hongjia Zhang, Lan Bai, Jun He, Lei Zhong, Xingmei Duan, Liang Ouyang, Yuxuan Zhu, Ting Wang, Yiwen Zhang, Jianyou Shi
Parkinson's disease (PD) is a common chronic degenerative disease of the central nervous system. Although the cause remains unknown, several pathological processes and central factors such as oxidative stress, mitochondrial injury, inflammatory reactions, abnormal deposition of α-synuclein, and cell apoptosis have been reported. Currently, anti-PD drugs are classified into two major groups: drugs that affect dopaminergic neurons and anti-cholinergic drugs. Unfortunately, the existing conventional strategies against PD are with numerous side effects, and cannot fundamentally improve the degenerative process of dopaminergic neurons...
September 30, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031069/synthesis-and-biological-evaluation-of-a-platinum-ii-c-rgdyk-conjugate-for-integrin-targeted-photodynamic-therapy
#3
T Chatzisideri, S Thysiadis, S Katsamakas, P Dalezis, I Sigala, T Lazarides, E Nikolakaki, D Trafalis, O A Gederaas, M Lindgren, V Sarli
A cancer-targeting conjugate 4 of a cyclometalated [N,C,N-Pt(II)] complex bearing a NˆCˆN 1,3-di(2-pyridyl)-benzene with c(RGDyK) peptide as guiding molecule was designed and synthesized for real-time drug delivery monitoring in cancer cells and photodynamic therapy (PDT). This conjugate demonstrates a mild cytostatic effect to six cancer cell lines expressing integrins at different extent, while possessing promising features for PDT. Conjugate 4 demonstrated rapid cell uptake by receptor-mediated endocytosis and efficient generation of (1)O2 upon irradiation...
September 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031066/serendipitous-discovery-of-potent-human-head-and-neck-squamous-cell-carcinoma-anti-cancer-molecules-a-fortunate-failure-of-a-rational-molecular-design
#4
Chiara Zagni, Venerando Pistarà, Luciana A Oliveira, Rogerio M Castilho, Giovanni Romeo, Ugo Chiacchio, Antonio Rescifina
Histone deacetylase inhibitors (HDACis) play an important role as valuable drugs targeted to cancer therapy: several HDACis are currently being tested in clinical trials. Two new potential HDACis 1a and 1d, characterized by the presence of a biphenyl-4-sulfonamide group as a connection unit between the N-{4-[(E)-(2-formylhydrazinylidene)methyl]-3-hydroxyphenyl} and the 2-hydroxy-N-(trifluoroacetyl)benzamide moiety, respectively, as two zinc-binding group (ZBG), have been designed, synthesized and tested for their biological activity...
October 5, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29031062/design-synthesis-and-biological-evaluations-of-n-hydroxy-thienopyrimidine-2-4-diones-as-inhibitors-of-hiv-reverse-transcriptase-associated-rnase-h
#5
Jayakanth Kankanala, Karen A Kirby, Andrew D Huber, Mary C Casey, Daniel J Wilson, Stefan G Sarafianos, Zhengqiang Wang
Human immunodeficiency virus (HIV) reverse transcriptase (RT) associated ribonuclease H (RNase H) is the only HIV enzymatic function not targeted by current antiviral drugs. Although various chemotypes have been reported to inhibit HIV RNase H, few have shown significant antiviral activities. We report herein the design, synthesis and biological evaluation of a novel N-hydroxy thienopyrimidine-2,3-dione chemotype (11) which potently and selectively inhibited RNase H with considerable potency against HIV-1 in cell culture...
September 28, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29029351/development-and-application-of-a-dual-rat-and-human-ahr-activation-assay
#6
Martin R Brown, Helen Garside, Emma Thompson, Saseela Atwal, Chloe Bean, Tony Goodall, Michael Sullivan, Mark J Graham
Significant prolonged AHR activation, classically exhibited following exposure to TCDD (dioxin), can cause a variety of undesirable toxicological effects. Novel pharmaceutical chemistries also have the potential to cause activation of AHR and consequent toxicities in pre-clinical species and man. Previous methods either employed relatively expensive and low throughput primary hepatocyte dosing with PCR endpoint, or low resolution overexpressing reporter gene assays. We have developed, validated and applied an in vitro microtitre plate imaging-based medium throughput screening assay for the assessment of endogenous species-specific AHR activation potential via detection of induction of the surrogate transcriptional target Cytochrome P450 CYP1A1...
September 18, 2017: Toxicological Sciences: An Official Journal of the Society of Toxicology
https://www.readbyqxmd.com/read/29029236/first-in-human-experience-with-complete-integration-of-neuromodulation-device-within-a-customized-cranial-implant
#7
Chad R Gordon, Gabriel F Santiago, Judy Huang, Gregory K Bergey, Shuya Liu, Mehran Armand, Henry Brem, William S Anderson
BACKGROUND: Neuromodulation devices have the potential to transform modern day treatments for patients with medicine-resistant neurological disease. For instance, the NeuroPace System (NeuroPace Inc, Mountain View, California) is a Food and Drug Administration (FDA)-approved device developed for closed-loop direct brain neurostimulation in the setting of drug-resistant focal epilepsy. However, current methods require placement either above or below the skull in nonanatomic locations. This type of positioning has several drawbacks including visible deformities and scalp pressure from underneath leading to eventual wound healing difficulties, micromotion of hardware with infection, and extrusion leading to premature explantation...
October 6, 2017: Operative Neurosurgery (Hagerstown, Md.)
https://www.readbyqxmd.com/read/29029067/pharmacodynamics-of-fosfomycin-against-esbl-and-or-carbapenemase-producing-enterobacteriaceae
#8
Fiona Fransen, Kelly Hermans, Maria J B Melchers, Claudia C M Lagarde, Joseph Meletiadis, Johan W Mouton
Background: The increase in antibiotic resistance in Gram-negative bacteria and the limited therapeutic options due to the shortage of new antibiotics have increased the interest of the 'old' antibiotic fosfomycin in the treatment of infections. However, there are contradictory reports on the pharmacodynamics of and emergence of resistance to fosfomycin. Methods: Time-kill assays were performed with 11 ESBL-positive and 3 ESBL-negative strains, exposing the bacteria to 2-fold static concentrations from 0...
October 4, 2017: Journal of Antimicrobial Chemotherapy
https://www.readbyqxmd.com/read/29029015/an-experimental-study-comparing-the-respiratory-effects-of-tapentadol-and-oxycodone-in-healthy-volunteers
#9
R van der Schrier, K Jonkman, M van Velzen, E Olofsen, A M Drewes, A Dahan, M Niesters
Background: There is a clinical need for potent opioids that produce little or no respiratory depression. In the current study we compared the respiratory effects of tapentadol, a mu-opioid receptor agonist and noradrenaline reuptake inhibitor, and oxycodone, a selective mu-opioid receptor agonist. We hypothesize that tapentadol 100 mg has a lesser effect on the control of breathing than oxycodone 20 mg. Methods: Fifteen healthy volunteers were randomized to receive oral tapentadol (100 and 150 mg), oxycodone 20 mg or placebo immediate release tablets in a crossover double-blind randomized design...
October 4, 2017: British Journal of Anaesthesia
https://www.readbyqxmd.com/read/29028643/pharmacotherapy-of-borderline-personality-disorder-replacing-confusion-with-prudent-pragmatism
#10
Vladan Starcevic, Aleksandar Janca
PURPOSE OF REVIEW: The article aims to examine trends in the pharmacological treatment of borderline personality disorder (BPD) and shed more light on the attendant controversies. RECENT FINDINGS: Although specialized, BPD-centred psychotherapy is considered first-line treatment for BPD and no psychotropic drug has been licensed for BPD, medications are frequently prescribed in the management of this condition. Various classes of psychopharmacological agents are used for BPD and there is a prominent polypharmacy...
October 11, 2017: Current Opinion in Psychiatry
https://www.readbyqxmd.com/read/29028517/effect-of-carbamazepine-and-oxcarbazepine-on-serum-neuron-specific-enolase-in-focal-seizures-a-randomized-controlled-trial
#11
Rituparna Maiti, Biswa Ranjan Mishra, Soham Sanyal, Debadatta Mohapatra, Sansita Parida, Archana Mishra
Neuron-specific enolase (NSE) is the most investigated biomarker in the context of epilepsy and brain damage. The present study was conducted to investigate the change in serum NSE in patients with focal seizure and the effect of carbamazepine and oxcarbazepine on serum NSE. The present study is a randomized, open-label, parallel design clinical trial (ClinicalTrials.gov Identifier: NCT02705768) conducted on 60 patients of focal seizure. After recruitment, detailed history, clinical evaluations including Chalfont-National Hospital seizure severity scale (NHS3), Quality of Life in Epilepsy Inventory (QOLIE-31) and serum NSE estimation were done at baseline...
October 6, 2017: Epilepsy Research
https://www.readbyqxmd.com/read/29028489/assessment-of-types-of-synthetic-cannabinoids-in-narcotic-cases-assessed-by-the-council-of-forensic-medicine-between-2011-2015-ankara-turkey
#12
Ersin Göl, İsmet Çok
Synthetic cannabinoids mimic the effects of cannabis and are the largest and fastest growing class of newly appearing designer drugs. Reports have revealed that various types of synthetic cannabinoids are mixed with herbal substances. The present study investigated the herbal substance cases involving synthetic cannabinoids in Ankara and nearby cities in Turkey. Data were collected from the reports of synthetic cannabinoids that were analyzed between January 01, 2011 and December 31, 2015 in the Ankara Narcotic Department of the Council of Forensic Medicine at the request of the judicial authorities...
October 4, 2017: Forensic Science International
https://www.readbyqxmd.com/read/29028335/metallo-supramolecular-complexes-enantioselectively-eradicate-cancer-stem-cells-in-vivo
#13
Hongshuang Qin, Chuanqi Zhao, Yuhuan Sun, Jinsong Ren, Xiaogang Qu
Cancer stem cells (CSCs) are responsible for drug resistance, metastasis and recurrence of cancers. However, there is still no clinically approved drug that can effectively eradicate CSCs. Thus, it is crucial and important to develop specific CSC-targeting agents. Chiral molecular recognition of DNA plays an important role in rational drug design. Among them, poly-morphic telomeric G-quadruplex DNA has received much attention due to its significant roles in telomerase activity and chromosome stability. Herein, we find that one enantiomer of zinc-finger-like chiral metallohelices, [Ni2L3]4+-P, a telomeric G-quadruplex-targeting ligand, can preferentially reduce cell growth in breast CSCs compared to the bulk cancer cells...
October 13, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29028303/neutrophil-particle-interactions-in-blood-circulation-drive-particle-clearance-and-alter-neutrophil-responses-in-acute-inflammation
#14
Catherine A Fromen, William J Kelley, Margaret B Fish, Reheman Adili, Jeffery Noble, Mark J Hoenerhoff, Michael Holinstat, Omolola Eniola-Adefeso
Although nano- and microparticle therapeutics have been studied for a range of drug delivery applications, the presence of these particles in blood flow may have considerable and understudied consequences to circulating leukocytes, especially neutrophils, which are the largest human leukocyte population. The objective of this work was to establish if particulate drug carriers in circulation interfere with normal neutrophil adhesion and migration. Circulating blood neutrophils in vivo were found to be capable of rapidly binding and sequestering injected carboxylate-modified particles of both 2 µm and 0...
October 13, 2017: ACS Nano
https://www.readbyqxmd.com/read/29027787/detection-of-t4-polynucleotide-kinase-via-allosteric-aptamer-probe-platform
#15
Mingxuan Gao, Jingjing Guo, Yanling Song, Zhi Zhu, Chaoyong James Yang
As a vital enzyme in DNA phosphorylation and restoration, T4 polynuceotide kinase (T4 PNK) has aroused great interest in recent years. Numerous strategies have been established for highly sensitive detection of T4 PNK based on diverse signal amplification techniques. However, they often need sophisticated design, a variety of auxiliary reagents and enzymes, or cumbersome manipulations. Herein, we have designed a new kind of allosteric aptamer probe consisting of streptavidin aptamer (SA aptamer) and the complementary DNA (cDNA) for simple detection of T4 PNK without signal amplification and with minimized interference in complex biological samples...
October 13, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/29027773/perioperative-pain-management-in-cardiac-surgery-a-systematic-review
#16
Elena Bignami, Alberto Castella, Vincenzo Pota, Francesco Saglietti, Antonio Scognamiglio, Cinzia Trumello, Maria C Pace, Massimo Allegri
BACKGROUND: Every year, more than 1.5 million patients, who undergo cardiac surgery worldwide, are exposed to a series of factors that can trigger acute postoperative pain associated with hemodynamic instability, respiratory complications, and psychological disorders. Through an evaluation of literature data about postoperative pain in cardiac surgery we define unmet needs and potential objectives for future research on this often underestimated problem. METHODS: Following PRISMA Guidelines, a systematic literature search was carried out by two independent researchers on Scopus, CINAHL, the Cochrane Library, and PubMed using the keywords: [(perioperative OR postoperative) analgesia AND "cardiac surgery"]...
October 12, 2017: Minerva Anestesiologica
https://www.readbyqxmd.com/read/29027412/-research-advances-in-secondary-development-of-chinese-patent-medicines-based-on-quality-by-design-concept
#17
Xing-Chu Gong, Teng Chen, Hai-Bin Qu
Quality by design (QbD) concept is an advanced pharmaceutical quality control concept. The application of QbD concept in the research and development of pharmaceutical processes of traditional Chinese medicines (TCM) mainly contains five parts, including the definition of critical processes and their evaluation criteria, the determination of critical process parameters and critical material attributes, the establishment of quantitative models, the development of design space, as well as the application and continuous improvement of control strategy...
March 2017: Zhongguo Zhong Yao za Zhi, Zhongguo Zhongyao Zazhi, China Journal of Chinese Materia Medica
https://www.readbyqxmd.com/read/29027350/liposome-encapsulated-chemotherapy-current-evidence-for-its-use-in-companion-animals
#18
REVIEW
B Børresen, A E Hansen, A Kjaer, T L Andresen, A T Kristensen
Cytotoxic drugs encapsulated into liposomes were originally designed to increase the anticancer response, while minimizing off-target adverse effects. The first liposomal chemotherapeutic drug was approved for use in humans more than 20 years ago, and the first publication regarding its use in a canine cancer patient was published shortly thereafter. Regardless, no general application for liposomal cytotoxic drugs has been established in veterinary oncology till now. Due to the popularity of canines as experimental models for pharmacokinetic analyses and toxicity studies, multiple publications exist describing various liposomal drugs in healthy dogs...
October 13, 2017: Veterinary and Comparative Oncology
https://www.readbyqxmd.com/read/29027137/cubic-liquid-crystalline-gels-based-on-glycerol-monooleate-for-intra-articular-injection
#19
Qian Li, Jiaojiao Cao, Zhengguang Li, Xiaoqin Chu
In situ gels containing sinomenine hydrochloride (SMH) for intra-articular (IA) administration to treat rheumatoid arthritis (RA) were designed and investigated in this study. Glycerol monooleate (GMO) was used due to the potential to generate viscous crystalline phase structures upon water absorption. The gels were evaluated using different parameters: syringeability, gelation, viscosity, and drug release. And, polarized light microscopy (PLM), small-angle X-ray scattering investigation (SAXS), and rheological studies were used to analyze their internal structures...
October 12, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/29027056/curcumin-affords-neuroprotection-and-inhibits-%C3%AE-synuclein-aggregation-in-lipopolysaccharide-induced-parkinson-s-disease-model
#20
Neha Sharma, Bimla Nehru
Parkinson's disease (PD) pathology is characterized by the abnormal accumulation and aggregation of the pre-synaptic protein α-synuclein in the dopaminergic neurons as Lewy bodies (LBs). Curcumin, which plays a neuroprotective role in various animal models of PD, was found to directly modulate the aggregation of α-synuclein in in vitro as well as in in vivo studies. While curcumin has been shown to exhibit strong anti-oxidant and anti-inflammatory properties, there are a number of other possible mechanisms by which curcumin may alter α-synuclein aggregation which still remains obscure...
October 12, 2017: Inflammopharmacology
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