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https://www.readbyqxmd.com/read/27775608/discovery-of-potent-carbonic-anhydrase-and-acetylcholinesterase-inhibitors-2-aminoindan-%C3%AE-lactam-derivatives
#1
Hayriye Genç, Ramazan Kalin, Zeynep Köksal, Nastaran Sadeghian, Umit M Kocyigit, Mustafa Zengin, İlhami Gülçin, Hasan Özdemir
β-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. β-Lactams were synthesized from benzylidene-inden derivatives and acetoxyacetyl chloride. The inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The results reveal that β-lactams are inhibitors of hCA I, II and AChE. The Ki values of β-lactams (2a-k) were 0.44-6.29 nM against hCA I, 0.93-8.34 nM against hCA II, and 0...
October 20, 2016: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/27673434/novel-dimer-compounds-that-bind-%C3%AE-synuclein-can-rescue-cell-growth-in-a-yeast-model-overexpressing-%C3%AE-synuclein-a-possible-prevention-strategy-for-parkinson-s-disease
#2
Joe Kakish, Kevin J H Allen, Troy A Harkness, Ed S Krol, Jeremy S Lee
The misfolding of α-synuclein is a critical event in the death of dopaminergic neurons and the progression of Parkinson's disease. Previously, it was suggested that drugs, which bind to α-synuclein and form a loop structure between the N- and C-termini, tend to be neuroprotective, whereas others, which cause a more compact structure, tend to be neurotoxic. To improve the binding to α-synuclein, eight novel compounds were synthesized from a caffeine scaffold attached to (R,S)-1-aminoindan, (R,S)-nicotine, and metformin, and their binding to α-synuclein determined through nanopore analysis and isothermal titration calorimetry...
October 7, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27606885/discovery-and-optimization-of-1-phenoxy-2-aminoindanes-as-potent-selective-and-orally-bioavailable-inhibitors-of-the-na-h-exchanger-type-3-nhe3
#3
Nils Rackelmann, Hans Matter, Heinrich Englert, Markus Follmann, Thomas Maier, John Weston, Petra Arndt, Winfried Heyse, Katharina Mertsch, Klaus Wirth, Laurent Bialy
The design, synthesis, and structure-activity relationship of 1-phenoxy-2-aminoindanes as inhibitors of the Na(+)/H(+) exchanger type 3 (NHE3) are described based on a hit from high-throughput screening (HTS). The chemical optimization resulted in the discovery of potent, selective, and orally bioavailable NHE3 inhibitors with 13d as best compound, showing high in vitro permeability and lacking CYP2D6 inhibition as main optimization parameters. Aligning 1-phenoxy-2-aminoindanes onto the X-ray structure of 13d then provided 3D-QSAR models for NHE3 inhibition capturing guidelines for optimization...
October 13, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27401914/study-on-the-metabolism-of-5-6-methylenedioxy-2-aminoindane-mdai-in-rats-identification-of-urinary-metabolites
#4
Monika Židková, Igor Linhart, Marie Balíková, Michal Himl, Lubomír Váňa, Michal Vetýška, Tomáš Páleníček, Eva Lhotková, Martin Dušek
1. 5,6-Methylenedioxy-2-aminoindane (MDAI) is a member of aminoindane drug family with serotoninergic effect, which appeared on illicit drug market as a substitute for banned stimulating and entactogenic drugs. 2. Metabolism of MDAI, which has been hitherto unexplored, was studied in rats dosed with a subcutaneous dose of 20 mg MDAI.HCl/kg body weight. The urine of rats was collected within 24 h after dosing for analyses by HPLC-ESI-HRMS and GC/MS. 3. The main metabolic pathways proceeding in parallel were found to be oxidative demethylenation followed by O-methylation and N-acetylation...
July 12, 2016: Xenobiotica; the Fate of Foreign Compounds in Biological Systems
https://www.readbyqxmd.com/read/27384665/structure-activity-relationships-of-the-human-immunodeficiency-virus-type-1-maturation-inhibitor-pf-46396
#5
Christopher Murgatroyd, Lisa Pirrie, Fanny Tran, Terry K Smith, Nicholas J Westwood, Catherine S Adamson
UNLABELLED: HIV-1 maturation inhibitors are a novel class of antiretroviral compounds that consist of two structurally distinct chemical classes: betulinic acid derivatives and the pyridone-based compound PF-46396. It is currently believed that both classes act by similar modes of action to generate aberrant noninfectious particles via inhibition of CA-SP1 cleavage during Gag proteolytic processing. In this study, we utilized a series of novel analogues with decreasing similarity to PF-46396 to determine the chemical groups within PF-46396 that contribute to antiviral activity, Gag binding, and the relationship between these essential properties...
September 15, 2016: Journal of Virology
https://www.readbyqxmd.com/read/27083855/emerging-toxicity-of-5-6-methylenedioxy-2-aminoindane-mdai-pharmacokinetics-behaviour-thermoregulation-and-ld50-in-rats
#6
Tomáš Páleníček, Eva Lhotková, Monika Žídková, Marie Balíková, Martin Kuchař, Michal Himl, Petra Mikšátková, Martin Čegan, Karel Valeš, Filip Tylš, Rachel R Horsley
MDAI (5,6-Methylenedioxy-2-aminoindane) has a reputation as a non-neurotoxic ecstasy replacement amongst recreational users, however the drug has been implicated in some severe and lethal intoxications. Due to this, and the fact that the drug is almost unexplored scientifically we investigated a broad range of effects of acute MDAI administration: pharmacokinetics (in sera, brain, liver and lung); behaviour (open field; prepulse inhibition, PPI); acute effects on thermoregulation (in group-/individually-housed rats); and systemic toxicity (median lethal dose, LD50) in Wistar rats...
August 1, 2016: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/27075859/chiral-bicyclic-bridgehead-phosphoramidite-briphos-ligands-for-asymmetric-rhodium-catalyzed-1-2-and-1-4-addition
#7
Ansoo Lee, Hyunwoo Kim
A complementary solution for Rh-catalyzed enantioselective 1,2- and 1,4-arylation with two structurally related chiral ligands is reported. A chiral bicyclic bridgehead phosphoramidite (briphos) ligand derived from 1-aminoindane was efficient for the 1,2-arylation of N-sulfonyl imines, while that derived from 1,2,3,4-tetrahydro-1-naphthylamine was efficient for 1,4-arylation of α,β-unsaturated cyclic ketones. For α,β-unsaturated N-tosyl ketimines, the briphos derived from 1-aminoindane was found to selectively provide γ,γ-diaryl N-tosyl enamines with high yields and stereoselectivities...
May 6, 2016: Journal of Organic Chemistry
https://www.readbyqxmd.com/read/27060436/simultaneous-bioanalysis-of-rasagiline-and-its-major-metabolites-in-human-plasma-by-lc-ms-ms-application-to-a-clinical-pharmacokinetic-study
#8
Ting Wang, Leting Yang, Jing Hua, Huiru Xie, Xuehua Jiang, Ling Wang
Rasagiline is a selective, irreversible inhibitor of monoamine oxidase type-B (MAO-B) and has been used both as a monotherapy and in addition to levodopa in the treatment of Parkinson's disease (PD). Rasagiline is metabolized by the cytochrome P450 (CYP) system, and the following three major metabolites with potential neuroprotective activity have been identified: 1-aminoindan (AI), 3-hydroxy-N-propargyl-1-aminoindan (3-OH-PAI) and 3-hydroxy-1-aminoindan (3-OH-AI). In this study, a novel liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed for the simultaneous determination of rasagiline and its major metabolites in human plasma...
June 5, 2016: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/27028902/locomotor-discriminative-stimulus-and-place-conditioning-effects-of-mdai-in-rodents
#9
Michael B Gatch, Sean B Dolan, Michael J Forster
5,6-Methylenedioxy-2-aminoindane (MDAI) has become a common substitute for (±)-3,4-methylenedioxymethamphetamine (MDMA) in Ecstasy. MDAI is known to produce MDMA-like discriminative stimulus effects, but it is not known whether MDAI has psychostimulant or hallucinogen-like effects. MDAI was tested for locomotor stimulant effects in mice and subsequently for discriminative stimulus effects in rats trained to discriminate cocaine (10 mg/kg, intraperitoneally), methamphetamine (1 mg/kg, intraperitoneally), ±MDMA (1...
September 2016: Behavioural Pharmacology
https://www.readbyqxmd.com/read/26951202/pharmacokinetics-of-rasagiline-in-healthy-adult-chinese-volunteers-with-various-genotypes-a-single-center-open-label-multiple-dose-study
#10
Xia Chen, Qian Zhao, Ji Jiang, Jian Liu, Pei Hu
BACKGROUND AND OBJECTIVE: Although there is evidence indicating cytochome P450 (CYP) 1A2 is responsible for the metabolism of rasagiline, the role of other CYP isoforms is unclear. This study investigated the pharmacokinetics of rasagiline in adult Chinese healthy volunteers with various CYP genotypes. METHODS: This single-center, open-label study was conducted in 12 subjects. Fasted subjects received rasagiline 1 mg daily for 7 days. Blood samples were taken to determine plasma concentrations of rasagiline, its major metabolite R-1-aminoindan (AI), and the genotyping of CYP2D6 and CYP2C19...
May 2016: Clinical Drug Investigation
https://www.readbyqxmd.com/read/26874736/a-snapshot-on-nps-in-italy-distribution-of-drugs-in-seized-materials-analysed-in-an-italian-forensic-laboratory-in-the-period-2013-2015
#11
Sara Odoardi, Francesco Saverio Romolo, Sabina Strano-Rossi
The diffusion of New Psychoactive Substances (NPS) in the illicit drug market is a worldwide problem. The aim of the study is to describe the qualitative distribution of drugs of abuse in seized materials confiscated in the Italian territory over the last two years. Between 2013 and 2015 162 seizures of substances purchased through the Internet and confiscated by police authorities were analyzed: 35 seizures (22%) were crystals of 3-methylmethcathinone (3-MMC). Although 3-MMC is subject to the relevant legislation in Italy, it is not controlled in other countries such as the Netherlands, from which the shipments originated...
August 2016: Forensic Science International
https://www.readbyqxmd.com/read/26791601/in-vitro-characterization-of-psychoactive-substances-at-rat-mouse-and-human-trace-amine-associated-receptor-1
#12
COMPARATIVE STUDY
Linda D Simmler, Danièle Buchy, Sylvie Chaboz, Marius C Hoener, Matthias E Liechti
Trace amine-associated receptor 1 (TAAR1) has been implicated in the behavioral effects of amphetamine-type stimulant drugs in rodents. TAAR1 has also been suggested as a target for novel medications to treat psychostimulant addiction. We previously reported that binding affinities at TAAR1 can differ between structural analogs of psychostimulants, and species differences have been observed. In this study, we complement our previous findings with additional substances and the determination of functional activation potencies...
April 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/26701297/metabotropic-glutamate-receptors-are-involved-in-the-detection-of-imp-and-l-amino-acids-by-mouse-taste-sensory-cells
#13
S Pal Choudhuri, R J Delay, E R Delay
G-protein-coupled receptors are thought to be involved in the detection of umami and L-amino acid taste. These include the heterodimer taste receptor type 1 member 1 (T1r1)+taste receptor type 1 member 3 (T1r3), taste and brain variants of mGluR4 and mGluR1, and calcium sensors. While several studies suggest T1r1+T1r3 is a broadly tuned lLamino acid receptor, little is known about the function of metabotropic glutamate receptors (mGluRs) in L-amino acid taste transduction. Calcium imaging of isolated taste sensory cells (TSCs) of T1r3-GFP and T1r3 knock-out (T1r3 KO) mice was performed using the ratiometric dye Fura 2 AM to investigate the role of different mGluRs in detecting various L-amino acids and inosine 5' monophosphate (IMP)...
March 1, 2016: Neuroscience
https://www.readbyqxmd.com/read/26607251/bdnf-levels-are-increased-by-aminoindan-and-rasagiline-in-a-double-lesion-model-of-parkinson-s-disease
#14
Aurélie Ledreux, Heather A Boger, Vanessa K Hinson, Kelsey Cantwell, Ann-Charlotte Granholm
The anti-Parkinsonian drug rasagiline is a selective, irreversible inhibitor of monoamine oxidase and is used in the treatment of Parkinson׳s disease (PD). Its postulated neuroprotective effects may be attributed to MAO inhibition, or to its propargylamine moiety. The major metabolite of rasagiline, aminoindan, has shown promising neuroprotective properties in vitro but there is a paucity of studies investigating in vivo effects of this compound. Therefore, we examined neuroprotective effects of rasagiline and its metabolite aminoindan in a double lesion model of PD...
January 15, 2016: Brain Research
https://www.readbyqxmd.com/read/26337076/synergistic-effect-of-antioxidant-system-and-osmolyte-in-hydrogen-sulfide-and-salicylic-acid-crosstalk-induced-heat-tolerance-in-maize-zea-mays-l-seedlings
#15
Zhong-Guang Li
Salicylic acid (SA), is a plant hormone with multifunction that is involved in plant growth, development and the acquisition of stress tolerance. Hydrogen sulfide (H2S) is emerging similar functions, but crosstalk between SA and H2S in the acquisition of heat tolerance is not clear. Our recent study firstly reported that SA treatment enhanced the activity of L-cysteine desulfhydrase (L-DES), a key enzyme in H2S biosynthesis, followed by induced endogenous H2S accumulation, which in turn improved the heat tolerance of maize seedlings...
2015: Plant Signaling & Behavior
https://www.readbyqxmd.com/read/26313846/asymmetric-pd-catalyzed-alkene-carboamination-reactions-for-the-synthesis-of-2-aminoindane-derivatives
#16
Derick R White, Johnathon T Hutt, John P Wolfe
A new type of Pd-catalyzed alkene carboamination reaction that provides direct access to enantioenriched 2-aminoindanes from 2-allylphenyltriflate derivatives and aliphatic amines is described. A catalyst generated in situ from Pd(OAc)2 and (S)-tert-butylPHOX provides the functionalized carbocycles in good yield with up to >99:1 er. The transformations occur via a key anti-aminopalladation that involves intermolecular attack of an amine nucleophile on an arylpalladium alkene complex.
September 9, 2015: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/26301619/rhodium-catalyzed-asymmetric-1-4-addition-of-%C3%AE-%C3%AE-unsaturated-imino-esters-using-chiral-bicyclic-bridgehead-phosphoramidite-ligands
#17
Ansoo Lee, Hyunwoo Kim
A chiral bicyclic bridgehead phosphoramidite (briphos) prepared from 1-aminoindane is a highly efficient and selective ligand for rhodium(I)-catalyzed asymmetric 1,4-addition of arylboronic acids to α,β-unsaturated N,N-dimethyl-sulfamoyl imino esters at ambient temperature. This transformation provides a new class of chiral (Z)-γ,γ-diaryl-α,β-dehydroamino esters with excellent yield and enantioselectivity.
September 9, 2015: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/26299055/-novel-central-dopaminergic-agents-derived-from-atypical-di-substituted-2-aminoindane-4-7-synthesis-and-central-pharmacological-profile
#18
Rosa Elena Ferrer-Mavárez, Noribel Coromoto Urdaneta-Gutierrez, Nicole Porta-Knabenschuh, Lucía Chiquinquirá Rodríguez-Villasmil, Cecire Carolina Rosales-Peña, Gustavo Adolfo Espinoza, Ligia Biagina Angel-Migliore, Katherin del Carmen Balza-Jiménez, Luis Eduardo Perdomo-Zavarce, Andrés Rafael Faría-Quintero, Akram Samear Dabian-Makarem, Mariana Vanessa Zapata-Cárdenas, Aarón Raúl Linero-Arrieta, Gustavo Adolfo Acurero-Castellano, Anita Israel-Stern, María Rosario Garrido, Heberto Suárez-Roca, Biagina del Carmen Migliore de Angel, Simón Enrique Lopez-D'Sola, Jaime Charris-Charris, María Matilde Ramírez-Moran, Jorge Eduardo Angel-Guío
In recent decades, many compounds with central dopaminergic activity have been designed, synthesized and evaluated pharmacologically. However, it has not been possible to obtain a drug able to improve or cure diseases involving dopaminergic regulation in the central nervous system, such as Parkinson's disease and schizophrenia, among others. Taking into consideration the term "atypical pharmacophore" and from the compound 5, the aralkyl fragment was incorporated, and the compounds 10, 11, 13a-h and 14a-h were synthesized...
June 2015: Investigación Clínica
https://www.readbyqxmd.com/read/26218505/studies-of-a-pyridino-crown-ether-based-chiral-stationary-phase-on-the-enantioseparation-of-biogenic-chiral-aralkylamines-and-%C3%AE-amino-acid-esters-by-high-performance-liquid-chromatography
#19
Sándor Lévai, Tamás Németh, Tamás Fődi, József Kupai, Tünde Tóth, Péter Huszthy, György Tibor Balogh
This paper reports the enantioseparation ability of a pyridino-18-crown-6 ether-based chiral stationary phase [(S,S)-CSP-1]. The enantiomeric discrimination of chiral stationary phase (S,S)-CSP-1 was evaluated by HPLC using the mixtures of enantiomers of various protonated primary aralkylamines [1-phenylethylamine hydrogen perchlorate (PEA), 2,3-dihydro-1H-inden-1-amine (1-aminoindan), 2,2'-(1,2-diaminoethane-1,2-diyl) diphenol (HPEN)] and perchlorate salts of α-amino acid esters [alanine benzyl ester (Ala-OBn), phenylalanine benzyl ester (Phe-OBn), phenylalanine methyl ester (Phe-OMe), phenylglycine methyl ester (PhGly-OMe), glutamic acid dibenzyl ester (Glu-diOBn), and valine benzyl ester (Val-OBn)]...
November 10, 2015: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/26102088/forensic-electrochemistry-indirect-electrochemical-sensing-of-the-components-of-the-new-psychoactive-substance-synthacaine
#20
Loanda R Cumba, Athanasios V Kolliopoulos, Jamie P Smith, Paul D Thompson, Peter R Evans, Oliver B Sutcliffe, Devaney R do Carmo, Craig E Banks
"Synthacaine" is a New Psychoactive Substance which is, due to its inherent psychoactive properties, reported to imitate the effects of cocaine and is therefore consequently branded as "legal cocaine". The only analytical approach reported to date for the sensing of "Synthacaine" is mass spectrometry. In this paper, we explore and evaluate a range of potential analytical techniques for its quantification and potential use in the field screening "Synthacaine" using Raman spectroscopy, presumptive (colour) testing, High Performance Liquid Chromatography (HPLC) and electrochemistry...
August 21, 2015: Analyst
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