Search results for "reo"
showing 10 items of 7464 documents
Horses Could Perceive Riding Differently Depending on the Way They Express Poor Welfare in the Stable
2020
International audience; This study investigated the relationships between four behavioral and postural indicators of a compromised welfare state in loose boxes (stereotypies, aggressive behaviors toward humans, withdrawn posture reflecting unresponsiveness to the environment, and alert posture indicating hypervigilance) and the way horses perceived riding. This perception was inferred using a survey completed by the usual riding instructor and during a standardized riding session (assessment of behaviors and postures, qualitative behavior assessment (QBA) and characterization of the horses' locomotion using an inertial measurement unit). In accordance with ear and tail positions and the QBA…
Asymmetric synthesis of 3,3′-pyrrolidinyl-dispirooxindoles via a one-pot organocatalytic Mannich/deprotection/aza-Michael sequence
2016
Chemical communications 52, 2249-2252 (2016). doi:10.1039/C5CC10057G
SYNTHESIS AND ANTITUMOR ACTIVITY OF 2,5-BIS(3'-INDOLYL)-FURANS AND 3,5-BIS(3'-INDOLIY)-ISOXAZOLES, NORTOPSENTIN ANALOGUES
2010
Abstract A series of novel 2,5-bis(3′-indolyl)furans and 3,5-bis(3′-indolyl)isoxazoles were synthesized as antitumor agents. The antiproliferative activity was evaluated in vitro toward diverse human tumor cell lines. Initially 5 isoxazoles and 3 furan derivatives were tested against a panel of 10 human tumor cell lines and the most active derivatives 3c and 4a were selected to be evaluated in an extended panel of 29 cell lines. By exhibiting mean IC50 values of 17.4 μg/mL (3a) and 20.5 μg/mL (4c), in particular 4c showed a high level of tumor selectivity toward the 29 cell lines.
Chiral Serum Pharmacokinetics of 4-Fluoroamphetamine after Controlled Oral Administration
2021
Abstract Over the last two decades, misuse of 4-fluoroamphetamine (4-FA) became an emerging issue in many European countries. Stimulating effects last for 4–6 hours and can impact psychomotor performance. The metabolism of amphetamine-type stimulants is stereoselective and quantification of (R)- and (S)-enantiomers has been suggested for assessing time of use. To date, no data on enantioselective pharmacokinetics is available for 4-FA in serum samples. An enantioselective liquid chromatography−tandem mass spectrometry (LC–MS-MS) method was developed using a chiral Phenomenex® Lux 3 μm AMP column. Validation of the method showed satisfactory selectivity, sensitivity, linearity (0.5–250 ng/mL…
Pyrido[2’,3’:4,5]pyrrolo[2,1-d][1,2,3,5]tetrazine-4(3H)-ones, a new class of temozolomide heteroanalogues
2009
Twelve derivatives of new ring system pyrido[2’,3’:4,5]pyrrolo[2,1-d][1,2,3,5]tetrazine were prepared in good yields by reaction of 2-diazo-3-ethoxycarbonyl-pyrrolo[3,2-b]pyridine with alkyl- or aryl-isocyanates. Nine derivatives, screened by the National Cancer Institute (Bethesda, MD) for the in vitro one dose primary anticancer assay against a panel of about 60 human tumor cell lines, showed no significant activity.
Diastereoselective synthesis of 6-functionalized 4-aryl-1,3-oxazinan-2-ones and their application in the synthesis of 3-aryl-1,3-aminoalcohols and 6-…
2010
Abstract Halocyclocarbamation of benzyl N -(1-phenyl-3-butenyl)carbamates afforded 6-functionalized 4-aryl-1,3-oxazinan-2-ones with moderate to excellent diastereoselectivity depending on the N -substituent. Importantly, in contrast to reported cyclocarbamations of homoallylic carbamates, which are generally trans -diastereoselective, cyclization of N -unsubstituted Cbz-protected homoallylamines led to cis -1,3-oxazinan-2-ones, predominantly. The use of N -benzylated and in situ prepared N -silylated derivatives resulted however in trans -selectivity. Transition states are proposed to explain the stereochemical influence of the N -substituent on the cyclocarbamations. The functionalized 1,3…
Enhanced field-of-view integral imaging display using multi-Köhler illumination.
2014
A common drawback in 3D integral imaging displays is the appearance of pseudoimages beyond the viewing angle. These pseudoimages appear when the light rays coming from each elemental image are not passing through the corresponding microlens, and a set of barriers must be used to avoid this flipping effect. We present a pure optical arrangement based on Köhler illumination to generate these barriers thus avoiding the pseudoimages. The proposed system does not use additional lenses to project the elemental images, so no optical aberrations are introduced. As an added benefit, Köhler illumination provides a higher contrast 3D display. This work was supported in part by the Plan Nacional I + D …
Synthesis of New 2-{[(Phenoxy or Phenyl)acetyl]amino}benzoic Acid Derivatives as 3α-Hydroxysteroid Dehydrogenase Inhibitors and Potential Antiinflamm…
1995
A number of 2-([(phenoxy or phenyl)acetyl]amino)benzoic acid derivatives were prepared in about 50% yield from (phenoxy or phenyl)acetyl chloride and anthranilic acid derivatives. All the compounds were tested as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase, since enzyme inhibition predicts potential antiinflammatory activity in vivo. The most active compounds 3 l, m, s are about 3.5 times more active than acetylsalicylic acid (ASA). Activity is influenced by electronic as well as steric effects.
“Twin” phosphorous atoms of tetraethyl 2-methyl-piperyd-1-ylmethylenebisphosphonates
2007
Recently, bisaminophosphonates found applications as therapeutic agents for curing bone disorders. When trying to relate the structures of substituted piperid-1-ylmethylenebisphosphonic with their biological properties, non-typical findings that in 31P NMR spectra of 2-methyl-piperid-1-ylmethylenebisphosphonic and 2-ethyl-piperid-1-ylmethylenebisphosphonic acids, two separate singlets from each of the phosphonic groups were observed, while their analogues bearing substituent in position 3 exhibit only one signal. Their presence was explained by freezing of the molecular motions by strong hydrogen bonding between NH and P = O atoms. In this work, synthesis as well as spectroscopic and theore…
The emerging role of 3D printing in the fabrication of detection systems
2021
Abstract 3D printing is fast evolving as an additive manufacturing technique that has been adopted in (bio)analytical science because of the ample variety of materials and technologies currently available for highly affordable prototyping. This review focuses on the unique characteristics of 3D printing for manufacturing of optical and electrochemical detection systems, and sampling interfaces for analytical purposes using fused deposition modelling, vat polymerization (stereolithography and digital light processing) and photopolymer inkjet printing. The majority of works surveyed within the time span of mid-2018 to mid-2020 encompassed the fabrication of several components of the detection…