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https://www.readbyqxmd.com/read/29345908/a-small-molecule-inhibitor-of-human-dna-polymerase-eta-potentiates-the-effects-of-cisplatin-in-tumor-cells
#1
Maroof K Zafar, Leena Maddukuri, Amit Ketkar, Narsimha Penthala, Megan R Reed, Sarah D Eddy, Peter A Crooks, Robert L Eoff
Translesion DNA synthesis (TLS) performed by human DNA polymerase eta (hpol η) allows tolerance of damage from cis-diamminedichloroplatinum(II) (CDDP or cisplatin). We have developed hpol η inhibitors derived from N-aryl-substituted indole barbituric acid (IBA), indole thiobarbituric acid (ITBA), and indole quinuclidine scaffolds and identified 5-((5-chloro-1-(naphthalen-2-ylmethyl)-1H-indol-3-yl)methylene)-2-thioxodihydropyrimidine-4,6(1H,5H)-dione (PNR-7-02), an ITBA derivative that inhibited hpol η activity with an IC50 value of 8 μM and exhibited five- to ten-fold specificity for hpol η over replicative pols...
January 18, 2018: Biochemistry
https://www.readbyqxmd.com/read/29336461/new-di-anchoring-a-%C3%AF-d-%C3%AF-a-configured-organic-chromophores-for-dssc-application-sensitization-and-co-sensitization-studies
#2
Praveen Naik, Rui Su, Mohamed R Elmorsy, Ahmed El-Shafei, Airody Vasudeva Adhikari
Herein, we report the design and synthesis of three new un-symmetrical metal-free carbazole based organic dyes, E1-3 with A-π-D-π-A architecture, as effective di-anchoring sensitizers in DSSCs. The new entities comprise carbazole as a donor scaffold connected to three different units, viz. cyano acetic acid, 2,4-thiazolidinedione and barbituric acid as acceptor/anchoring units via vinylene and phenylene as π-spacers at 3- and 6-positions of the carbazole ring, respectively. Photophysical, electrochemical and theoretical studies were carried out in order to assess their feasibility as active sensitizers...
January 16, 2018: Photochemical & Photobiological Sciences
https://www.readbyqxmd.com/read/29334621/taurine-as-a-green-bio-organic-catalyst-for-the-preparation-of-bio-active-barbituric-and-thiobarbituric-acid-derivatives-in-water-media
#3
Nader Daneshvar, Farhad Shirini, Mohaddeseh Safarpoor Nikoo Langarudi, Reyhaneh Karimi-Chayjani
Taurine, a β-amino acid that is abundantly available in the tissues of human and animals, is efficiently used as a green bio-organic catalyst in the preparation of some of the biologically active barbituric and thiobarbituric acid derivatives. In the presence of taurine, 5-Arylidene (thio) barbituric acid derivatives were prepared via Knovenagel reaction between aldehydes and (thio)barbituric acid. Using this reagent also pyrano[2,3-d]pyrimidinone(thione) derivatives were synthesized through a three-component reaction between aldehydes, (thio)barbituric and malononitrile...
December 21, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29318302/a-one-pot-multicomponent-reaction-for-the-synthesis-of-oligoetherols-with-azacyclic-rings
#4
Jacek Lubczak, Renata Lubczak, Iwona Zarzyka
The one-pot multicomponent synthesis of oligoetherols containing azacycles is described. They were obtained by reaction of isocyanuric, barbituric, or uric acid or melamine with glycidol and alkylene carbonates. The isolated products were characterized by physical methods and their properties were compared with the same compounds obtained in twostep protocol. The oligoetherols with 1,3,5-triazine ring obtained by both methods were then used to form polyurethane foams and their properties were compared.
December 2017: Acta Chimica Slovenica
https://www.readbyqxmd.com/read/29286885/stability-of-pentobarbital-in-soil
#5
Chasity Bagsby, Anita Saha, Granville Goodin, Sheeba Siddiqi, Mary Farone, Anthony Farone, Paul C Kline
Intravenous injection of barbiturates, particularly pentobarbital (5-ethyl-5-pentan-2-yl-1,3-diazinane-2,4,5-trione), is a widely used method to euthanize large animals such as horses. However, one concern with this method is the fate of pentobarbital after the disposal of the carcass. As tissues decompose, pentobarbital may leach into the soil and from there migrate to groundwater. A method using methanol extraction, solid phase concentration, and liquid chromatography (LC/MS) has been developed to measure pentobarbital in soils...
December 29, 2017: Journal of Environmental Science and Health. Part. B, Pesticides, Food Contaminants, and Agricultural Wastes
https://www.readbyqxmd.com/read/29276297/patient-outcomes-associated-with-phenobarbital-use-with-or-without-benzodiazepines-for-alcohol-withdrawal-syndrome-a-systematic-review
#6
Drayton A Hammond, Jordan M Rowe, Adrian Wong, Tessa L Wiley, Kristen C Lee, Sandra L Kane-Gill
Purpose: Benzodiazepines are the drug of choice for alcohol withdrawal syndrome (AWS); however, phenobarbital is an alternative agent used with or without concomitant benzodiazepine therapy. In this systematic review, we evaluate patient outcomes with phenobarbital for AWS. Methods: Medline, Cochrane Library, and Scopus were searched from 1950 through February 2017 for controlled trials and observational studies using ["phenobarbital" or "barbiturate"] and ["alcohol withdrawal" or "delirium tremens."] Risk of bias was assessed using tools recommended by National Heart, Lung, and Blood Institute...
October 2017: Hospital Pharmacy
https://www.readbyqxmd.com/read/29250413/buthalital-and-methitural-5-5-substituted-derivatives-of-2-thio-barbituric-acid-forming-the-same-type-of-hydrogen-bonded-chain
#7
Thomas Gelbrich, Ulrich J Griesser
The mol-ecule of buthalital, (I) [systematic name: 5-(2-methyl-prop-yl)-5-(prop-2-en-1-yl)-2-sulfanyl-idene-1,3-diazinane-4,6-dione], C11H16N2O2S, exhibits a planar pyrimidine ring, whereas the pyrimidine ring of methitural, (II) [systematic name: 5-(1-methyl-but-yl)-5-[2-(methyl-sulfan-yl)eth-yl]-2-sulfanyl-idene-1,3-diazinane-4,6-dione], C12H20N2O2S2, is slightly puckered. (I) and (II) contain the same hydrogen-bonded chain structure in which each mol-ecule is connected, via four N-H⋯O=C hydrogen bonds, to two other mol-ecules, resulting in a hydrogen-bonded chain displaying a sequence of R22(8) rings...
December 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/29248688/application-of-silica-coated-magnetite-nanoparticles-modified-with-cu-i-neocuproine-as-nanosorbent-to-simultaneous-separation-preconcentration-of-trace-amounts-of-nitrate-and-nitrite
#8
Rasool Roohparvar, Tayebeh Shamspur, Ali Mostafavi
A novel, inexpensive and sensitive type of magnetic nanosorbent based on the functionalized silica-coated Fe3O4 nanoparticles was prepared and used for the adsorption of trace amounts of nitrite and nitrate ions. The work is based on selective ion-pairing complex formation of nitrate and nitrite with Cu(I)-neocuproine which are covalently bounded on nanoparticles. Nitrite was determined according to its reaction with barbituric acid to give violuric acid and determination of nitrate was based on its reduction to nitrite in the presence of Zn/NaCl...
December 14, 2017: Nitric Oxide: Biology and Chemistry
https://www.readbyqxmd.com/read/29244082/quantitation-of-cocaine-and-metabolites-phencyclidine-butalbital-and-phenobarbital-in-meconium-by-liquid-chromatography-tandem-mass-spectrometry
#9
Triniti L Scroggin, Gwendolyn A McMillin
In this study, a quantitative polarity switching liquid chromatography coupled with a tandem mass spectrometer (LC-MS/MS) method was developed to detect and quantify cocaine and metabolites (cocaethylene, benzoylecgonine and meta-hydroxybenzoylecgonine), phencyclidine (PCP) and barbiturates (phenobarbital and butalbital) in meconium. Accuracy and precision samples at 0.0125% and 75% of the upper limit of quantitation (ULOQ) were analyzed in triplicate over 5 days with accuracy above 84% and average %CV values below 11%...
December 13, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/29227273/-poisoning-by-psychopharmacological-drugs-in-azerbaijan-the-results-of-8-year-prospective-observation
#10
I Afandiyev, V Azizov
Acute poisoning of chemical etiology is a significant global public health problem. The aim of this study was the analysis of the toxicoepidemiological structure of psychopharmacological drugs poisoning in Azerbaijan. We collected and analyzed the data on all cases of acute poisoning by psychopharmacological drugs (codes of categories T42/T43 ICD-10) undergoing inpatient treatment at the Center of Clinical Toxicology in Baku, Azerbaijan in 2009-2016. The total number of patients with acute intoxication by psychopharmacological drugs was 3,413, which was 48...
November 2017: Georgian Medical News
https://www.readbyqxmd.com/read/29223098/trisubstituted-barbiturates-and-thiobarbiturates-synthesis-and-biological-evaluation-as-xanthine-oxidase-inhibitors-antioxidants-antibacterial-and-anti-proliferative-agents
#11
Joana Figueiredo, João L Serrano, Eunice Cavalheiro, Leena Keurulainen, Jari Yli-Kauhaluoma, Vânia M Moreira, Susana Ferreira, Fernanda C Domingues, Samuel Silvestre, Paulo Almeida
Barbituric and thiobarbituric acid derivatives have become progressively attractive to medicinal chemists due to their wide range of biological activities. Herein, different series of 1,3,5-trisubstituted barbiturates and thiobarbiturates were prepared in moderate to excellent yields and their activity as xanthine oxidase inhibitors, antioxidants, antibacterial agents and as anti-proliferative compounds was evaluated in vitro. Interesting bioactive barbiturates were found namely, 1,3-dimethyl-5-[1-(2-phenylhydrazinyl)ethylidene]pyrimidine-2,4,6(1H,3H,5H)-trione (6c) and 1,3-dimethyl-5-[1-[2-(4-nitrophenyl)hydrazinyl]ethylidene]pyrimidine-2,4,6(1H,3H,5H)-trione (6e), which showed concomitant xanthine oxidase inhibitory effect (IC50 values of 24...
November 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29207675/thio-barbiturate-derived-compounds-are-novel-antioxidants-to-prevent-lps-induced-inflammation-in-the-liver
#12
Kyoung Mi Moon, Bonggi Lee, Ji Won Jeong, Dae Hyun Kim, Yun Jung Park, Hye Rim Kim, Ji Young Park, Min Jo Kim, Hye Jin An, Eun Kyeong Lee, Young Mi Ha, Eunok Im, Pusoon Chun, Jin Yeul Ma, Won-Kyung Cho, Hyung Ryong Moon, Hae Young Chung
Liver inflammation is closely associated with metabolic syndrome. Oxidative stress plays a synergistic role in inflammation by activating nuclear factor kappa B (NF-κB) signaling in the liver. Therefore, substantial efforts have been made to develop compounds that inhibit the generation of oxidative stress and activation of NF-κB. We synthesized twenty-six novel 5-(substituted benzyl)-2-oxo- and 5-(substituted benzyl)-2-thioxo-dihydropyrimidine-4,6(1H,5H)-dione derivatives for the development of potential antioxidants and examined their biological activities in vitro and in vivo...
October 31, 2017: Oncotarget
https://www.readbyqxmd.com/read/29180889/risk-of-respiratory-depression-with-opioids-and-concomitant-gabapentinoids
#13
Julie Savelloni, Heather Gunter, Kelly C Lee, Chih Hsu, Cassia Yi, Kyle P Edmonds, Timothy Furnish, Rabia S Atayee
Introduction: The combination of opioids and central nervous system depressants such as benzodiazepines and barbiturates has an additive effect on the frequency of oversedation and respiratory depression requiring naloxone use in hospitalized patients. Gabapentinoids (gabapentin and pregabalin) are frequently prescribed with opioids for their opioid-sparing and adjuvant analgesic effects. There is limited literature on the risk of respiratory depression due to the combination of opioids and gabapentinoids requiring naloxone administration...
2017: Journal of Pain Research
https://www.readbyqxmd.com/read/29165453/structural-and-electronic-properties-of-barbituric-acid-and-melamine-containing-ribonucleosides-as-plausible-components-of-prebiotic-rna-implications-for-prebiotic-self-assembly
#14
Sarabjeet Kaur, Purshotam Sharma, Stacey D Wetmore
The RNA world hypothesis assumes that RNA was the first informational polymer that originated from prebiotic chemical soup. However, since the reaction of d-ribose with canonical nucleobases (A, C, G and U) fails to yield ribonucleosides (rNs) in substantial amounts, the spontaneous origin of rNs and the subsequent synthesis of RNA remains an unsolved mystery. To this end, it has been suggested that RNA may have evolved from primitive genetic material (preRNA) composed of simpler prebiotic heterocycles that spontaneously form glycosidic bonds with ribose...
November 22, 2017: Physical Chemistry Chemical Physics: PCCP
https://www.readbyqxmd.com/read/29162023/pentobarbital-removal-during-continuous-venovenous-hemofiltration-case-report-and-review-of-the-literature
#15
David M Hensler, Deepika P McConnell, Kimberly E Levasseur-Franklin, Kasey M Greathouse
BACKGROUND: Renal replacement therapy may enhance the elimination of barbiturates. Pentobarbital clearance during continuous venovenous hemofiltration (CVVH) has not been described previously. We report a patient case involving the measurement of serial pentobarbital levels during CVVH and review relevant literature characterizing extracorporeal pentobarbital elimination. METHODS: The following is a retrospective report of a previously healthy 26-year-old woman who sustained a severe traumatic brain injury (TBI) and required administration of pentobarbital on hospital day 0 for intracranial pressure (ICP) control...
January 1, 2017: Journal of Pharmacy Practice
https://www.readbyqxmd.com/read/29160806/synthesis-of-nitrogen-heterocycles-using-samarium-ii-iodide
#16
REVIEW
Shicheng Shi, Michal Szostak
Nitrogen heterocycles represent vital structural motifs in biologically-active natural products and pharmaceuticals. As a result, the development of new, convenient and more efficient processes to N-heterocycles is of great interest to synthetic chemists. Samarium(II) iodide (SmI₂, Kagan's reagent) has been widely used to forge challenging C-C bonds through reductive coupling reactions. Historically, the use of SmI₂ in organic synthesis has been focused on the construction of carbocycles and oxygen-containing motifs...
November 21, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29155148/functional-properties-and-mechanism-of-action-of-pptq-an-allosteric-agonist-and-low-nanomolar-positive-allosteric-modulator-at-gabaa-receptors
#17
Nawid Madjroh, Emma Rie Olander, Christoffer Bundgaard, Pella Cecilia Söderhielm, Anders A Jensen
The former sedative-hypnotic and recreational drug methaqualone (Quaalude) is a moderately potent, non-selective positive allosteric modulator (PAM) at GABAA receptors (GABAARs) (Hammer et al., 2015). In the present study, we have identified a novel methaqualone analog, 2-phenyl-3-(p-tolyl)quinazolin-4(3H)-one (PPTQ), in a screening of 67 analogs at five αβ2γ2S GABAAR subtypes and delineated its functional properties and mechanism of action at wild-type and mutant GABAARs expressed in Xenopus laevis oocytes by two-electrode voltage clamp electrophysiology...
January 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/29147507/gelation-driven-selection-in-dynamic-covalent-c-0000000000000000000000000000000000-0000000000000000000000000000000000-0000000000000000000000000000000000-0000000000000000000000000000000000-0000000000000000000000000000000000-0000000000000000000000000000000000
#18
Chunshuang Liang, Sirinan Kulchat, Shimei Jiang, Jean-Marie Lehn
Knoevenagel barbiturate derivatives bearing long alkyl chains were proven to form organogels in suitable solvents based on supramolecular interactions. Their reaction with imines allows for component exchange through CC/CN recombination. The effect of various parameters (solvents, chain length, and temperature) on the CC/CN exchange reaction has been studied. Mixing Knoevenagel compound K and imine I-16 in a 1 : 1 ratio generated a constitutional dynamic library containing the four constituents K, I-16, K'-16, and I'...
October 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/29142416/protective-effect-of-pluchea-lanceolata-against-aluminum-chloride-induced-neurotoxicity-in-swiss-albino-mice
#19
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
#20
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
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