Search results for "stereo"

Synthesis and anti-HIV activity of 2,3-diaryl-1,3-thiazolidin-4-(thi)one derivatives.

2002

Several 2,3-diaryl-1,3-thiazolidine-4-thione derivatives and 2,3-diaryl-1,3-thiazolidin-4-ones bearing a methyl group at C-5 position have been synthesized and tested as anti-HIV agents. The results of the in vitro tests showed that some of them proved to be effective inhibitors of HIV-1 replication.

Synthesis of disparlure and monachalure enantiomers from 2,3-butanediacetals

2020

2,3-Butanediacetal derivatives were used for the stereoselective synthesis of unsymmetrically substituted cis-epoxides. The procedure was applied for the preparation of both enantiomers of disparlure and monachalure, the components of the sex pheromones of the gypsy moth (Lymantria dispar) and the nun moth (Lymantria monacha) using methyl (2S,3R,5R,6R)-3-ethylsulfanylcarbonyl-5,6-dimethoxy-5,6-dimethyl-1,4-dioxane-2-carboxylate as the starting material.

Preparation and structural characterization of organotin(IV) complexes with ligands containing a hetero {N} atom and a hydroxy group or hydroxy and c…

2005

AbstractTwenty-two n-butyltin(IV) and t-butyltin(IV) complexes of ligands containing an –OH (–C@O) group or –OH and –COOHgroups and an aromatic {N} donor atom were prepared by metathetical reactions. On the basis of the FT-IR and Mo¨ssbauer spec-troscopic data, molecular structures were assigned to these compounds. The binding sites of the ligands were identified by means ofFT-IR spectroscopic measurements, and it was found that in most cases the organotin(IV) moiety reacts with the phenolic form ofthese ligands. In the complexes with –OH and –COOH functions, the –COOH group is coordinated to the organotin(IV) centres in amonodentate manner. The 119 Sn Mo¨ssbauer and the FT-IR studies suppor…

ChemInform Abstract: Regio- and Stereoselective Addition of Grignard Reagents to N-Galactosyl-2-pyridone: Synthesis of 4-Substituted 5,6-Didehydro-2-…

2010

NO donors. Part 16: investigations on structure-activity relationships of organic mononitrates reveal 2-nitrooxyethylammoniumnitrate as a high potent…

2007

The vasoactive properties of 14 organic mononitrates were investigated in vitro using PGF(2alpha)-precontracted porcine pulmonary arteries. A surprisingly wide range of vasorelaxant potencies was observed (pD(2): 3.36-7.50). Activities showed to be highly sensitive to the molecular structure and the substituents at the molecular carrier of the nitrate group. A correlation between lipophilicity and vasorelaxant potency could not be recognized. 2-Nitrooxyethylammoniumnitrate (1) was found to be slightly superior to the high potency trinitrate GTN.

Intercultural crisis communication during the 2011 Fukushima nuclear disaster

2014

With the motivation of contributing to further development of the emerging field of intercultural crisis communication, the study aims at exploring the reasons why the global media criticized the Japanese authorities’ crisis communication during the 2011 Fukushima nuclear disaster through the inductive content analysis on both the Japanese authorities’ crisis communication and the global media’s perceptions on the Japanese authorities’ crisis communication. The data collected from 11 March to September 2011, including 160 press releases, transcripts of the foreign press conferences and speeches delivered at the international conferences by the Japanese authorities, and 120 news reports from…

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…