keyword
MENU ▼
Read by QxMD icon Read
search

drug substitution

keyword
https://www.readbyqxmd.com/read/28821122/-click-hyaluronan-based-nanohydrogels-as-multifunctionalizable-carriers-for-hydrophobic-drugs
#1
Giuliana Manzi, Nicole Zoratto, Silvia Matano, Rocchina Sabia, Claudio Villani, Tommasina Coviello, Pietro Matricardi, Chiara Di Meo
Highly hydrophilic and biocompatible nanocarriers based on polysaccharide hydrogels (nanohydrogels, NHs) were shown to be promising systems for drug delivery applications. Following the idea of these emerging drug carriers, the aim of the present work was to develop self-assembled hydrogel nanoparticles based on amphiphilic derivatives of hyaluronic acid (HA) and riboflavin (Rfv), synthesized by "click" Copper(I)-catalyzed Azide-Alkyne Cycloaddition (CuAAC) reaction. The obtained amphiphilic product (HA-c-Rfv) was able to form nanohydrogels in aqueous environments, in particular by applying an innovative autoclave-based method...
October 15, 2017: Carbohydrate Polymers
https://www.readbyqxmd.com/read/28820579/site-specific-conjugation-to-native-and-engineered-lysines-in-human-immunoglobulins-by-microbial-transglutaminase
#2
Jared Spidel, Benjamin Vaessen, Earl Albone, Xin Cheng, Arielle Verdi, J Bradford Kline
The use of microbial transglutaminase (MTG) to produce site-specific antibody-drug conjugates (ADCs) has thus far focused on transamidation of engineered acyl donor glutamine residues in an antibody based on the hypothesis that the lower specificity of MTG for acyl acceptor lysines may result in transamidation of multiple native lysine residues, thereby yielding heterogeneous products. We investigated the utilization of native IgG lysines as acyl acceptor sites for glutamine-based acyl donor substrates. Of the approximately 80 lysines in multiple recombinant IgG monoclonal antibodies (mAbs), none were transamidated...
August 18, 2017: Bioconjugate Chemistry
https://www.readbyqxmd.com/read/28818724/enzyme-sensitive-smart-inulin-dehydropeptide-conjugate-self-assembles-into-nanostructures-useful-for-targeted-delivery-of-ornidazole
#3
Kriti Shivhare, Charu Garg, Ayushi Priyam, Alka Gupta, Ashwani Kumar Sharma, Pradeep Kumar
Molecular self-assembly of biodegradable amphiphilic polymers allows rational design of biocompatible nanomaterials for drug delivery. Use of substituted polysaccharides for such applications offers the ease of design and synthesis, and provides higher biofunctionality and biocompatibility to nanomaterials. The present work focuses on the synthesis, characterization and potential biomedical applications of self-assembled polysaccharide-based materials. We demonstrated that the synthesized amphiphilic inulin self-assembled in aqueous medium into nanostructures with average size in the range of 146-486nm and encapsulated hydrophobic therapeutic molecule, ornidazole...
August 14, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28818114/the-impact-of-subsidized-low-aromatic-fuel-laf-on-petrol-gasoline-sniffing-in-remote-australian-indigenous-communities
#4
Peter d'Abbs, Gillian Shaw, Emma Field
BACKGROUND: Since 2005, the Australian Government has subsidized the production and distribution of Low Aromatic Fuel (LAF) as a deterrent against petrol (gasoline) sniffing in remote Indigenous communities. LAF is used in place of unleaded petrol as a fuel for vehicles and other engines. This paper reports findings from an independent evaluation of the LAF rollout. METHODS: Forty one Indigenous communities were surveyed between 2010 and 2014, with each community being visited twice at a two yearly interval...
August 17, 2017: Substance Abuse Treatment, Prevention, and Policy
https://www.readbyqxmd.com/read/28817222/heavily-substituted-atropisomeric-diarylamines-by-unactivated-smiles-rearrangement-of-n-aryl-anthranilamides
#5
Romain Costil, Harvey Dale, Natalie Fey, George Whitcombe, Johnathan Matlock, Jonathan Clayden
Diarylamines find use as metal ligands and as structural components of drug molecules, and are commonly made by metal catalyzed C-N coupling. However, the limited tolerance to steric hindrance of these couplings restricts the synthetic availability of more substituted diarylamines. Here we report a remarkable variant of the Smiles rearrangement that employs readily accessible N-aryl anthranilamides as precursors to diarylamines. Conformational predisposition of the anthranilamide starting material brings the aryl rings into proximity and allows the rearrangement to take place despite the absence of electron-withdrawing substituents, and even with sterically encumbered doubly ortho-substituted substrates...
August 17, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28815279/evaluation-of-training-dose-in-male-sprague-dawley-rats-trained-to-discriminate-4-methylmethcathinone
#6
Michael D Berquist, Nathyn A Thompson, Lisa E Baker
RATIONALE: Although the synthetic cathinone 4-methylmethcathinone (4-MMC, mephedrone) has been a subject of intensive research investigation, the pharmacological mechanisms involved in its interoceptive stimulus effects have yet to be fully characterized. OBJECTIVE: The present study employed drug discrimination methods in rats to compare the interoceptive stimulus properties of two different training doses of 4-MMC to other substances with similar pharmacological actions...
August 16, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28814513/escape-of-tick-borne-flavivirus-from-2-c-methylated-nucleoside-antivirals-is-mediated-by-a-single-conservative-mutation-in-ns5-that-has-a-dramatic-effect-on-viral-fitness
#7
Ludek Eyer, Hirofumi Kondo, Darina Zouharova, Minato Hirano, James J Valdés, Memi Muto, Tomas Kastl, Shintaro Kobayashi, Jan Haviernik, Manabu Igarashi, Hiroaki Kariwa, Marketa Vaculovicova, Jiri Cerny, Rene Kizek, Andrea Kröger, Stefan Lienenklaus, Milan Dejmek, Radim Nencka, Martin Palus, Jiri Salat, Erik De Clercq, Kentaro Yoshii, Daniel Ruzek
Tick-borne encephalitis virus (TBEV) causes a severe and potentially fatal neuroinfection in humans. Despite its high medical relevance, no specific antiviral therapy is currently available. Here we demonstrate that treatment with a nucleoside analog, 7-deaza-2' -C-methyladenosine (7-deaza-2' -CMA), substantially improved disease outcome, increased survival, and reduced signs of neuroinfection and viral titers in the brains of mice infected with a lethal dose of TBEV. To investigate the mechanism of action of 7-deaza-2' -CMA, two drug-resistant TBEV clones were generated and characterized...
August 16, 2017: Journal of Virology
https://www.readbyqxmd.com/read/28810741/photochemical-synthesis-of-3-azabicyclo-3-2-0-heptanes-advanced-building-blocks-for-drug-discovery
#8
Aleksandr V Denisenko, Tetiana Druzhenko, Yevhen Skalenko, Maryna Samoilenko, Oleksandr O Grygorenko, Sergey Zozulya, Pavel K Mykhailiuk
We have developed a rapid two-step synthesis of substituted 3 azabicyclo[3.2.0]heptanes which are attractive building blocks for drug discovery. This new method utilizes very common chemicals - benzaldehyde, allylamine and cinnamic acid, - via intramolectular [2+2] photochemical cyclization.
August 16, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28810188/novel-tacrine-derivatives-exhibiting-improved-acetylcholinesterase-inhibition-design-synthesis-and-biological-evaluation
#9
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
https://www.readbyqxmd.com/read/28807917/bedaquiline-inhibits-the-atp-synthase-in-mycobacterium-abscessus-and-is-effective-in-infected-zebrafish
#10
Christian Dupont, Albertus Viljoen, Sangeeta Thomas, Françoise Roquet-Banères, Jean-Louis Herrmann, Kevin Pethe, Laurent Kremer
Pulmonary infections caused by Mycobacterium abscessus are emerging as a global threat, especially in cystic fibrosis patients. Further intensifying the concern of M. abscessus infection is the recent evidence of human-to-human transmission of the infection. M. abscessus is a naturally multidrug resistant, fast-growing pathogen for which pharmacological options are limited. Repurposing antitubercular drugs represents an attractive option for the development of chemotherapeutic alternatives against M. abscessus infections...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807908/activity-of-the-%C3%AE-lactamase-inhibitor-ln-1-255-against-carbapenem-hydrolyzing-class-d-%C3%AE-lactamases-from-acinetobacter-baumannii
#11
Juan Carlos Vázquez-Ucha, María Maneiro, Marta Martínez-Guitián, John Buynak, Christopher R Bethel, Robert A Bonomo, Germán Bou, Margarita Poza, Concepción González-Bello, Alejandro Beceiro
The number of infections caused by Gram-negative pathogens carrying carbapenemases is increasing, and the group of carbapenem-hydrolyzing class D β-lactamases (CHDLs) is especially problematic. Several clinically important CHDLs have been identified in A. baumannii, including OXA-23, OXA-24/40, OXA-58, OXA-143, OXA-235, and the chromosomally encoded OXA-51. The selection and dissemination of carbapenem-resistant A. baumannii strains constitutes a serious global threat. Carbapenems have been successfully utilized as last resort antibiotics for the treatment of multi-drug-resistant A...
August 14, 2017: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/28807759/development-of-a-highly-resolved-loop-mediated-isothermal-amplification-method-to-detect-the-n526k-ftsi-mutation-of-%C3%AE-lactamase-negative-ampicillin-resistant-haemophilus-influenzae
#12
Shinsuke Tamura, Takuya Maeda, Kazuhisa Misawa, Morichika Osa, Takaaki Hamamoto, Atsushi Yuki, Kazuo Imai, Kei Mikita, Kyoko Morichika, Akihiko Kawana, Hiroshi Matsumoto, Shigeaki Nonoyama
Rapid and easy detection of sequence polymorphisms, including nucleotide point mutations of bacterial pathogens responsible for amino acid substitutions linked to drug resistance, is essential for the proper use of antimicrobial agents. Here, a detection method using loop-mediated amplification (LAMP) combined with amplification refractory mutation system (ARMS) to accurately distinguish a different single nucleotide in the target sequence was established, named ARMS-SNP LAMP. This procedure is capable of species-specific detection of a nucleotide (1578T) in the ftsI gene on Haemophilus influenzae without amplifying the sequence carrying the point mutations (T1578G/A) in β-lactamase-negative ampicillin resistant (BLNAR) strains...
August 11, 2017: Journal of Microbiological Methods
https://www.readbyqxmd.com/read/28807650/current-state-of-biosimilars-in-mexico-the-position-of-the-mexican-college-of-rheumatology-2016
#13
Daniel Xibille, Sandra Carrillo, Gabriela Huerta-Sil, Ramiro Hernández, Leonardo Limón, Guadalupe Olvera-Soto, Luis Javier Jara-Quezada, Abdieel Esquivel, Marcela Pérez-Rodríguez
The present document is a position statement of the Mexican College of Rheumatology on the use of biosimilars in rheumatic diseases. This position considers that biosimilars should be considered as interchangeable, that automatic substitution without previous notice in stable patients during follow-up is not ethical, that the approval of a biosimilar should only be given after exhaustive review of preclinical and clinical data marked by Mexican regulations, that it should be clearly stated in the nomenclature of biologic drugs which is the innovator and which is the biosimilar, that it is not correct to choose a biosimilar as treatment based only on economic reasons or extrapolate indications based only on the approval of the innovator and in the absence of safety and efficacy data for the biosimilar...
August 11, 2017: Reumatología Clinica
https://www.readbyqxmd.com/read/28807037/selepressin-a-novel-selective-vasopressin-v1a-agonist-is-an-effective-substitute-for-norepinephrine-in-a-phase-iia-randomized-placebo-controlled-trial-in-septic-shock-patients
#14
James A Russell, Jean-Louis Vincent, Anne Louise Kjølbye, Håkan Olsson, Allan Blemings, Herbert Spapen, Peder Carl, Pierre-Francois Laterre, Lars Grundemar
BACKGROUND: Vasopressin is widely used for vasopressor support in septic shock patients, but experimental evidence suggests that selective V1A agonists are superior. The initial pharmacodynamic effects, pharmacokinetics, and safety of selepressin, a novel V1A-selective vasopressin analogue, was examined in a phase IIa trial in septic shock patients. METHODS: This was a randomized, double-blind, placebo-controlled multicenter trial in 53 patients in early septic shock (aged ≥18 years, fluid resuscitation, requiring vasopressor support) who received selepressin 1...
August 15, 2017: Critical Care: the Official Journal of the Critical Care Forum
https://www.readbyqxmd.com/read/28806959/second-line-therapy-for-helicobacter-pylori-eradication-causing-antibiotic-associated-hemorrhagic-colitis
#15
Kazuyuki Tanaka, Mikihiro Fujiya, Aki Sakatani, Shugo Fujibayashi, Yoshiki Nomura, Nobuhiro Ueno, Shin Kashima, Takuma Goto, Junpei Sasajima, Kentaro Moriichi, Toshikatsu Okumura
OBJECTIVE: Helicobacter pylori (H. pylori) eradication rarely develops into antibiotic-associated hemorrhagic colitis (AAHC), in which the etiology of colitis remains unclear. We herein report a rare case of AAHC caused by second-line therapy for H. pylori eradication. RESULTS: A 65-year-old female was administered second-line therapy for H. pylori composed of 1500 mg of amoxicillin, 500 mg of metronidazole and 40 mg of vonoprazan for 7 days because of first-line therapy failure...
August 14, 2017: Annals of Clinical Microbiology and Antimicrobials
https://www.readbyqxmd.com/read/28805982/a-serious-nightmare-psychiatric-and-neurologic-adverse-reactions-to-mefloquine-are-serious-adverse-reactions
#16
Remington L Nevin
Mefloquine (originally marketed as Lariam) is a neurotoxic quinoline derivative antimalarial drug that is known to cause serious and potentially lasting neuropsychiatric adverse reactions. Since 2013, drug regulators in several jurisdictions, including the United States, the United Kingdom, Ireland, and Canada, have required their mefloquine labels be updated to warn that when used for malaria prophylaxis the drug should be discontinued at the onset of neurologic or psychiatric symptoms. These recent changes to the international labeling serve to imply that psychiatric and neurologic reactions to mefloquine prophylaxis may be an early warning of an impending more serious reaction that may further jeopardize the patient with continued use of the drug...
August 2017: Pharmacology Research & Perspectives
https://www.readbyqxmd.com/read/28804788/pro-dopamine-regulator-kb220-to-balance-brain-reward-circuitry-in-reward-deficiency-syndrome-rds
#17
Kenneth Blum, Marcelo Febo, Lyle Fried, David Baron, Eric R Braverman, Kristina Dushaj, Mona Li, Zsolt Demetrovics, Rajendra D Badgaiyan
We are faced with a worldwide opiate/opioid epidemic that is devastating. According to the Centers for Disease Control and Prevention (CDC), at least 127 people, young and old, are dying every day in America due to narcotic overdose. The Food and Drug Administration (FDA) has approved Medication-Assisted Treatments (MATs) for opiate/opioids as well as alcohol and nicotine. The mechanism of action of most MATS favors either blocking of dopaminergic function or a form of Opiate Substitution Therapy (OST). These treatment options are adequate for short-term treatment of the symptoms of addiction and harm reduction but fail long-term to deal with the cause or lead to recovery...
2017: Journal of Reward Deficiency Syndrome and Addiction Science
https://www.readbyqxmd.com/read/28803965/the-great-divide-separation-between-in-vitro-and-in-vivo-effects-of-psncbam-based-cb1-receptor-allosteric-modulators
#18
Thomas F Gamage, Charlotte E Farquhar, Timothy W Lefever, Brian F Thomas, Thuy Nguyen, Yanan Zhang, Jenny L Wiley
While allosteric modulators of the cannabinoid type-1 receptor (CB1) continue to be developed and characterized, the gap between the in vitro and in vivo data is widening, raising questions regarding translatability of their effects and biological relevance. Among the CB1 allosteric modulators, PSNCBAM-1 has received little attention regarding its effects in vivo. Recently, pregnenolone was reported to act as an allosteric modulator of CB1, blocking THC's effects in vitro and in vivo, highlighting the potential of CB1 allosteric modulators for treatment of cannabis intoxication...
August 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28802866/global-update-on-the-susceptibility-of-human-influenza-viruses-to-neuraminidase-inhibitors-2015-2016
#19
Larisa V Gubareva, Terry G Besselaar, Rod S Daniels, Alicia Fry, Vicki Gregory, Weijuan Huang, Aeron C Hurt, Patricia A Jorquera, Angie Lackenby, Sook-Kwan Leang, Janice Lo, Dmitriy Pereyaslov, Helena Rebelo-de-Andrade, Marilda M Siqueira, Emi Takashita, Takato Odagiri, Dayan Wang, Wenqing Zhang, Adam Meijer
Four World Health Organization (WHO) Collaborating Centres for Reference and Research on Influenza and one WHO Collaborating Centre for the Surveillance, Epidemiology and Control of Influenza (WHO CCs) assessed antiviral susceptibility of 14,330 influenza A and B viruses collected by WHO-recognized National Influenza Centres (NICs) between May 2015 and May 2016. Neuraminidase (NA) inhibition assay was used to determine 50% inhibitory concentration (IC50) data for NA inhibitors (NAIs) oseltamivir, zanamivir, peramivir and laninamivir...
August 9, 2017: Antiviral Research
https://www.readbyqxmd.com/read/28801098/synthesis-and-in-vitro-evaluation-of-ca-2-channel-blockers-1-4-dihydropyridines-analogues-against-trypanosoma-cruzi-and-leishmania-amazonensis-sar-analysis
#20
Luiz A E Pollo, Milene H de Moraes, Júlia Cisilotto, Tânia B Creczynski-Pasa, Maique W Biavatti, Mario Steindel, Louis P Sandjo
Drugs containing the1,4-dihydropyridine (DHP) core have recently attracted attention concerning their antiparasitic effect against various species of Leishmania and Trypanosoma. This approach named drugs repositioning led to interesting results, which have prompted us to prepare 21 DHP's analogues. The 1,4-DHP scaffold was decorated with different function groups at tree points including the nitrogen atom (NH and N-phenyl), the aryl group attached to C-4 (various substituted aryl residues) and the carbon atoms 2 and 6 (bearing Ph or Me groups)...
August 8, 2017: Parasitology International
keyword
keyword
38903
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"