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https://www.readbyqxmd.com/read/29142416/protective-effect-of-pluchea-lanceolata-against-aluminum-chloride-induced-neurotoxicity-in-swiss-albino-mice
#1
Ravi Mundugaru, Senthilkumar Sivanesan, Padmaja Udaykumar, Niranjan Rao, Naveen Chandra
Background: Aluminum chloride (AlCl3) is a known potent environmental neurotoxin causing progressive neurodegenerative changes in the brain. The herb Pluchea lanceolata is commonly known as "Rasana" and used as a nerve tonic in neuroinflammatory conditions in Indian system of medicine. Objective: To evaluate the neuroprotective activity of hydroalcoholic extract of P. lanceolata in chronic AlCl3-induced neurotoxicity in Swiss albino mice. Materials and Methods: Albino mice were categorized into four different groups; Group 1served as vehicle control, Group 2 mice were administered with AlCl3, 40 mg/kg body weight by intraperitoneal route for 45 consecutive days...
October 2017: Pharmacognosy Magazine
https://www.readbyqxmd.com/read/29141143/michael-michael-addition-reactions-promoted-by-secondary-amine-thiourea-stereocontrolled-construction-of-barbiturate-fused-tetrahydropyrano-scaffolds-and-pyranocoumarins
#2
Jing Zhang, Guohui Yin, Yuchao Du, Ziqi Yang, Yang Li, Ligong Chen
Bifunctional secondary amine-thiourea organocatalysts were successfully applied in the stereocontrolled synthesis of barbiturate fused tetrahydropyrano scaffold. As compared with the generally used tertiary amine-thiourea organocatalysts, they exhibited Bifunctional secondary amine-thiourea organocatalysts were successfully applied in the stereocontrolled synthesis of barbiturate-fused tetrahydropyrano scaffolds. Compared with typically used tertiary amine-thiourea organocatalysts, the developed catalysts exhibited excellent catalytic performance in the domino Michael-Michael reaction between N,N'-dimethylbarbituric acid and Morita-Baylis-Hillman acetates of nitroalkenes to yield pharmaceutically important heterocycles in good yields with excellent enantioselectivities...
November 15, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/29133035/design-and-synthesis-of-novel-thiobarbituric-acid-derivatives-targeting-both-wild-type-and-braf-mutated-melanoma-cells
#3
Srinivasa Rao Ramisetti, Manoj K Pandey, Sang Y Lee, Deepkamal Karelia, Satya Narayan, Shantu Amin, Arun K Sharma
A series of novel thio- and seleno-barbituric acid derivatives were synthesized by varying the substituents at N1 and N3 (ethyl, methyl, allyl, and phenyl), and C5 tethered with dienyl and trienyl moieties attached to substituents such as phenyl, 2-furanyl, 2-thiophenyl, 1-naphthyl, and 3-pyridyl. The cytotoxic potential of these derivatives was evaluated by using MTT assay against melanoma cell lines expressing either wild-type (CHL-1) or mutant (UACC 903) BRAF gene. Among all, 2b and 8b were identified as the most potent compounds...
November 4, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29124988/extracorporeal-elimination-of-butalbital-in-acute-aspirin-butalbital-caffeine-codeine-fiorinal-with-codeine-poisoning
#4
Janelle O Poyant, Robert Albright, Jeremy Clain, Govind Pandompatam, Erin F Barreto
BACKGROUND: Butalbital is a small molecule (approximately 220 Da), with 26% protein binding, a 0.8 L/kg volume of distribution, and is eliminated nearly 80% unchanged in the urine. Although hemodialysis has been used to treat overdoses of other barbiturates, the extracorporeal clearance of butalbital is unknown. The objective of this case is to describe the use of extracorporeal therapy to augment elimination of butalbital after an overdose of aspirin 325 mg-butalbital 50 mg-caffeine 40 mg with codeine 30 mg (Fiorinal with Codeine)...
November 10, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/29095046/molecular-spectroscopic-studies-examining-the-interactions-between-phenobarbital-and-human-serum-albumin-in-alcohol-consumption
#5
Sheng-Feng Cui, Wei Li, Cheng-He Zhou
BACKGROUND: Alcohol dependence is associated with a wide range of serious mental, physical, and social consequences and is one of the most common chronic diseases worldwide. Barbiturates, which are a first-line treatment in the clinic for alcohol withdrawal, may result in combined barbiturate and alcohol use. Their co-use abuse may promote synergistic effects between barbiturates and alcohol in vivo. OBJECTIVE: To investigate the effects of different alcohol concentrations on the synergistic effects of phenobarbital and alcohol...
November 2, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/29068170/antidote-availability-in-saudi-arabia-hospitals-in-the-riyadh-province
#6
Abdullah AlTamimi, Nidal K Malhis, Najla M Khojah, Saleh A Manea, Abdulrahman AlTamimi, Sami Ayed AlShammary
Inadequate antidote stocking is a global problem in hospitals. Insufficient supplies and delays in the administration of antidotes could lead to death and additional potentially negative clinical consequences. Our objective was to determine the availability of antidotes in hospitals listed on the Saudi Ministry of Health website in the Riyadh Province and to evaluate the leading poison in Saudi Arabia. A cross-sectional study was conducted using questionnaires. The questionnaires were distributed to pharmacist directors and emergency room-treating physicians in 17 public hospitals throughout the Riyadh Province...
October 25, 2017: Basic & Clinical Pharmacology & Toxicology
https://www.readbyqxmd.com/read/29058090/icp-management-in-patients-suffering-from-traumatic-brain-injury-a-systematic-review-of-randomized-controlled-trials
#7
REVIEW
Peter Abraham, Robert C Rennert, Brandon C Gabel, Jayson A Sack, Navaz Karanjia, Peter Warnke, Clark C Chen
BACKGROUND: Severe traumatic brain injury (sTBI) is a major cause of morbidity and mortality. Intracranial pressure (ICP) monitoring and management form the cornerstone of treatment paradigms for sTBI in developed countries. We examine the available randomized controlled trial (RCT) data on the impact of ICP management on clinical outcomes after sTBI. METHODS: A systematic review of the literature on ICP management following sTBI was performed to identify pertinent RCT articles...
December 2017: Acta Neurochirurgica
https://www.readbyqxmd.com/read/29050394/cortical-neurons-and-networks-are-dormant-but-fully-responsive-during-isoelectric-brain-state
#8
Tristan Altwegg-Boussac, Adrien E Schramm, Jimena Ballestero, Fanny Grosselin, Mario Chavez, Sarah Lecas, Michel Baulac, Lionel Naccache, Sophie Demeret, Vincent Navarro, Séverine Mahon, Stéphane Charpier
A continuous isoelectric electroencephalogram reflects an interruption of endogenously-generated activity in cortical networks and systematically results in a complete dissolution of conscious processes. This electro-cerebral inactivity occurs during various brain disorders, including hypothermia, drug intoxication, long-lasting anoxia and brain trauma. It can also be induced in a therapeutic context, following the administration of high doses of barbiturate-derived compounds, to interrupt a hyper-refractory status epilepticus...
September 1, 2017: Brain: a Journal of Neurology
https://www.readbyqxmd.com/read/29044798/the-impact-of-substance-use-disorders-on-clinical-outcomes-in-older-adult-psychiatric-inpatients
#9
Scott D Lane, Sabrina C da Costa, Antonio L Teixeira, Charles F Reynolds, Breno S Diniz
OBJECTIVE: To examine associations among substance use disorder (SUD) and measures of length of stay (LOS) and non-psychiatric medical comorbidity (MEDCO) in older-adult inpatients with serious mental illness (SMI), hypothesizing SUD would be related to worse clinical outcomes. METHODS: A cross-sectional study analyzed medical records from 2010 to 2016 of 7258 inpatients with SMI ≥ age 50, obtained from a 274-bed psychiatric hospital. Descriptive analyses examined prevalence rates for SUD status (+/-), individual drug classes, and total number of SUDs (polysubstance use disorders)...
October 18, 2017: International Journal of Geriatric Psychiatry
https://www.readbyqxmd.com/read/29023111/catalytic-asymmetric-synthesis-of-quaternary-barbituric-acids
#10
Sandra Del Pozo, Silvia Vera, Mikel Oiarbide, Claudio Palomo
The catalytic asymmetric α-functionalization of prochiral barbituric acids, a subtype of pseudosymmetric 1,3-diamides, to yield the corresponding 5,5-disubstituted (quaternary) derivatives remains essentially unsolved. In this study 2-alkylthio-4,6-dioxopirimidines are designed as key 1,3-diamide surrogates that perform exceedingly in amine-squaramide catalyzed C-C bond forming reactions with vinyl ketones or Morita-Baylis-Hillmann-type allyl bromides as electrophiles. Mild acid hydrolysis of adducts affords barbituric acid derivatives with an in-ring quaternary carbon in unprecedented enantioselectivity, offering valuable materials for biological evaluations...
October 17, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/29019682/synthesis-of-%C3%AE-ketosulfonamides-derived-from-amino-acids-and-their-conversion-to-%C3%AE-keto-%C3%AE-%C3%AE-difluorosulfonamides-via-electrophilic-fluorination
#11
Jacob Soley, Edmond Chiu, Ryan Chung, Jeremy Green, Jason E Hein, Scott D Taylor
β-Ketosulfonamides derived from Boc or Cbz-protected amino acids bearing hydrophobic side chains were prepared in good to excellent yield by treating N-allyl, N-alkyl methanesulfonamides with n-BuLi, followed by reaction of the resulting carbanion with methyl esters of N-protected l-amino acids. The analogous reaction using the dianion derived from an N-alkyl methanesulfonamide proceeded in much lower yield. Electrophilic fluorination of the β-ketosulfonamides using Selectfluor in the presence of CsF in DMF at room temperature for 15-60 min provided β-keto-α,α-difluorosulfonamides in good to excellent yields...
October 11, 2017: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/28990625/enantioselective-organocatalytic-michael-additions-of-n-n-dialkylbarbituric-acids-to-enones
#12
Ying Liu, Yongna Zhang, Hui-Xin Duan, Dong-Yan Wanyan, You-Qing Wang
N,N'-Dialkylbarbituric acids as cyclic malonamide donors were successfully used in the enantioselective Michael addition reaction of enones. Using cinchona alkaloid-based bifunctional squaramide as an organocatalyst, this Michael reaction of N,N'-di-tert-butylbarbituric acid with various enones features a highly enantioselective (91-99% ee) production of the corresponding optically active 5-substituted barbituric acid derivatives. The transformations of the Michael product for the barbituric acid structural unit were realized in two ways, deprotection to remove the N-tert-butyl group and alkylation to produce 5,5-disubstituted barbituric acid derivatives...
October 18, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28935856/sequence-controlled-supramolecular-terpolymerization-directed-by-specific-molecular-recognitions
#13
Takehiro Hirao, Hiroaki Kudo, Tomoko Amimoto, Takeharu Haino
Nature precisely manipulates primary monomer sequences in biopolymers. In synthetic polymer sequences, this precision has been limited because of the lack of polymerization techniques for conventional polymer synthesis. Engineering the primary monomer sequence of a polymer main chain represents a considerable challenge in polymer science. Here, we report the development of sequence-controlled supramolecular terpolymerization via a self-sorting behavior among three sets of monomers possessing mismatched host-guest pairs...
September 21, 2017: Nature Communications
https://www.readbyqxmd.com/read/28905718/physiologic-behavioral-and-histologic-responses-to-various-euthanasia-methods-in-c57bl-6ntac-male-mice
#14
Gregory P Boivin, Michael A Bottomley, Patricia A Schiml, Lori Goss, Nadja Grobe
Rodent euthanasia using exposure to increasing concentrations of CO2 has come under scrutiny due to concerns of potential pain during the euthanasia process. Alternatives to CO2, such as isoflurane and barbiturates, have been proposed as more humane methods of euthanasia. In this study, we examined 3 commonly used euthanasia methods in mice: intraperitoneal injection of pentobarbital-phenytoin solution, CO2 inhalation, and isoflurane anesthesia followed by CO2 inhalation. We hypothesized that pentobarbital-phenytoin euthanasia would cause fewer alterations in cardiovascular response, result in less behavioral evidence of pain or stress, and produce lower elevations in ACTH than would the isoflurane and CO2 methods, which we hypothesized would not differ in regard to these parameters...
January 1, 2017: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/28899906/does-the-doctrine-of-double-effect-apply-to-the-prescription-of-barbiturates-syme-vs-the-medical-board-of-australia
#15
Xavier Symons
The doctrine of double effect (DDE) is a principle of crucial importance in law and medicine. In medicine, the principle is generally accepted to apply in cases where the treatment necessary to relieve pain and physical suffering runs the risk of hastening the patient's death. More controversially, it has also been used as a justification for withdrawal of treatment from living individuals and physician-assisted suicide. In this paper, I will critique the findings of the controversial Victorian Civil and Administrative Tribunal (VCAT) hearing Syme vs the Medical Board of Australia In that hearing, Dr Rodney Syme, a urologist and euthanasia advocate, was defending his practice of prescribing barbiturates to terminally ill patients...
September 12, 2017: Journal of Medical Ethics
https://www.readbyqxmd.com/read/28894410/life-threatening-dyskalaemia-after-barbiturate-coma-therapy-the-strategy-of-management
#16
Yeap Boon Tat, Wan Mohd Nazaruddin Wan Hassan, Ting Yung Chuen, Abdul Rahman Izaini Ghani
Barbiturate coma therapy (BCT) is a treatment option that is used for refractory intracranial hypertension after all other options have been exhausted. Although BCT is a brain protection treatment, it also has several side effects such as hypotension, hepatic dysfunction, renal dysfunction, respiratory complications and electrolyte imbalances. One less concerning but potentially life-threatening complication of BCT is dyskalaemia. This complication could present as severe refractory hypokalaemia during the therapy with subsequent rebound hyperkalaemia after cessation of the therapy...
March 2017: Malaysian Journal of Medical Sciences: MJMS
https://www.readbyqxmd.com/read/28878016/enantiomeric-barbiturates-bind-distinct-inter-and-intrasubunit-binding-sites-in-a-nicotinic-acetylcholine-receptor-nachr
#17
Zhiyi Yu, Jonathan B Cohen
Nicotinic acetylcholine receptors (nAChRs) and γ-aminobutyric acid type A receptors (GABAARs) are members of the pentameric ligand-gated ion channel superfamily. Drugs acting as positive allosteric modulators of muscle-type α2βγδ nAChRs, of use in treatment of neuromuscular disorders, have been hard to identify. However, identification of nAChR allosteric modulator binding sites has been facilitated by using drugs developed as photoreactive GABAAR modulators. Recently, R-1-methyl-5-allyl-5-(m-trifluoromethyl-diazirinylphenyl) barbituric acid (R-mTFD-MPAB), an anesthetic and GABAAR potentiator, has been shown to inhibit Torpedo α2βγδ nAChRs, binding in the ion channel and to a γ(+)-α(-) subunit interface site similar to its GABAAR intersubunit binding site...
October 20, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28866270/small-molecule-inhibitors-of-bacterial-transcription-complex-formation
#18
Daniel S Wenholz, Ming Zeng, Cong Ma, Marcin Mielczarek, Xiao Yang, Mohan Bhadbhade, David St C Black, Peter J Lewis, Renate Griffith, Naresh Kumar
Knoevenagel condensation was employed to generate a set of molecules potentially capable of inhibiting the RNA polymerase-σ(70)/σ(A) interaction in bacteria. Synthesis was achieved via reactions between a variety of indole-7-carbaldehydes and rhodanine, N-allylrhodanine, barbituric acid or thiobarbituric acid. A library of structurally diverse compounds was examined by enzyme-linked immunosorbent assay (ELISA) to assess the inhibition of the targeted protein-protein interaction. Inhibition of bacterial growth was also evaluated using Bacillus subtilis and Escherichia coli cultures...
September 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28862044/acute-lamotrigine-overdose-a-systematic-review-of-published-adult-and-pediatric-cases
#19
Bader Alyahya, Marjorie Friesen, Bénédicte Nauche, Martin Laliberté
CONTEXT: Lamotrigine is a broad-spectrum anticonvulsant commonly used to treat seizure and bipolar mood disorders. Evidence from case series and retrospective studies indicate that lamotrigine overdose is usually benign. However, there are reported cases of cardiac arrest and mortality following lamotrigine overdose. We undertook a systematic review of the literature on lamotrigine overdoses to better understand the clinical severity, the relevance of serum concentrations, and therapeutic interventions for overdose...
September 1, 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28858148/alcohol-or-drug-use-and-trauma-recidivism
#20
COMPARATIVE STUDY
Sergio Cordovilla-Guardia, Raquel Vilar-López, Pablo Lardelli-Claret, Francisco Guerrero-López, Enrique Fernández-Mondéjar
BACKGROUND: Alcohol, illicit drugs, and psychotropic medications are well-known causes of traumatic events. However, the association of each type of substance with trauma recidivism remains unclear. OBJECTIVES: The purpose of this study was to quantify the strength of associations between the type of substance detected in patients admitted for traumatic injury and trauma recidivism, defined as a documented history of past trauma. METHODS: The presence of alcohol and drugs (cannabis, cocaine, amphetamines, methamphetamines, benzodiazepines, opiates, methadone, barbiturates, and tricyclic antidepressants) was analyzed in 1,156 patients between 16 and 70 years old, hospitalized in a trauma hospital between November 2011 and March 2015...
September 2017: Nursing Research
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