Search results for "Azocine"

Comparative studies of the Pschorr reaction in the pyrazole series. Access to the new dibenzo[e,g]pyrazolo[1,5-a][1,3]diazocine system of pharmaceuti…

2008

The diazonium tetrafluoroborate 11 obtained from 2-amino-N-methyl-N-(1-phenyl-3- methylpyrazol-5-yl)benzamide was transformed in dry acetonitrile via an ionic or radical pathway. Differences were observed with respect to ionic or radical transformations in aqueous media of the analogous diazonium hydrogen sulfate 1 derived from the same amine. In acetonitrile solution, the ionic pathway was characterized by an increased yield of 1,4-dimethyl- 3-phenyl-pyrazolo(3,4-c)isoquinolin-5-one 4 and by the formation of its isomer, the new derivative 7,9-dimethyldibenzo(e,g)pyrazolo(1,5-a)(1,3)diazocin-10(9H)-one 12. When the reaction followed a radical pathway, the pyrazolo(3,4-c)isoquinoline derivat…

Solvent-Enhanced Diastereo- and Regioselectivity in the PdII-Catalyzed Synthesis of Six- and Eight-Membered Heterocycles viacis-Aminopalladation

2009

The Pd(II)-catalyzed intramolecular oxidative cyclization of tosyl-protected cis- and trans-N-allyl-2-aminocyclohexanecarboxamides was examined, and efficient syntheses of cyclohexane-fused pyrimidin-4-ones and 1,5-diazocin-6-ones were developed. In the course of the research, a marked solvent effect was observed on both the regio- and diastereoselectivity. Additionally, a novel Pd(II)-mediated domino oxidation, oxidative amination reaction was discovered. Our experimental and theoretical findings suggest that the reactions proceed via a cis-aminopalladation mechanism.

A facile synthesis of 1-ethyl-3-methyl-11-phenyl-1,4-dihydro-5H-pyrazolo[3,4-c][1,5]benzodiazocin-5-ones.A new ring system.

2007

Verschiedene Opioide beim kardiovaskul�ren Risikopatienten

1994

Efficient analgesia may be the major objective in the cardiovascular risk patient following myocardial infarction, acute occlusion of peripheral vessels, or dissection/perforation of major abdominal vessels. It was the purpose of the study to investigate the haemodynamic and respiratory side effects of eight different opioids in 57 circulatory risk patients prior to major vascular surgery. Methods. Patients were randomly allocated to eight groups, each receiving a different opioid within a clinical, equipotent dose range (buprenorphine, fentanyl, morphine, nalbuphine, pentazocine, pethidine, tramadol, alfentanil). A complete haemodynamic and blood gas status was obtained prior to as well as…

Efficient Conversion of Light to Chemical Energy : Directional, Chiral Photoswitches with Very High Quantum Yields

2020

Abstract Photochromic systems have been used to achieve a number of engineering functions such as light energy conversion, molecular motors, pumps, actuators, and sensors. Key to practical applications is a high efficiency in the conversion of light to chemical energy, a rigid structure for the transmission of force to the environment, and directed motion during isomerization. We present a novel type of photochromic system (diindane diazocines) that converts visible light with an efficiency of 18 % to chemical energy. Quantum yields are exceptionally high with >70 % for the cis–trans isomerization and 90 % for the back‐reaction and thus higher than the biochemical system rhodopsin (64 %). T…

Synthesis of pyrazolo[4,3-c][1,2,6]benzothiadiazocine, a new ring system as potential COX inhibitor

2012

Derivatives of the new ring system 1,4-dihydropyrazolo[4,3-c][1,2,6] benzothiadiazocin-11(10H)one 5,5-dioxide were synthesized in five or six steps in 57-66% overall yields and tested as COX inhibitors.

Failure of opioids to affect excitation and contraction in isolated ventricular heart muscle

1989

The opioid agonists morphine (selective for mu-receptors) and ethylketocyclazocine (selective for kappa-receptors), at concentrations evoking strong effects in neuronal structures, did not significantly affect the configuration of the intracellularly recorded action potential and the force of contraction in ventricular heart muscle isolated from guinea pigs, rabbits and man. These results suggest that any changes of heart functions in vivo in response to opioid-like drugs are probably not mediated postsynaptically at the myocardial cell membrane but rather presynaptically, influencing the release of noradrenaline and/or acetylcholine from the nerve terminals.

Analgosedierungsverfahren f�r zahn�rztlich-chirurgische Eingriffe mit Midazolam/Pentazocin und Midazolam/Ketamin Klinische Doppelblindstudie zu Anxio…

1995

Ketamin/Midazolam zur Analgosedierung erwies sich in bezug auf Kreislauf und Atmung gegenuber Pentazocin/Midazolam uberlegen [23]. Diese Studie sollte klaren, ob 0,25 oder 0,5 mg/kg KG Ketamin, 0,075 mg/kg KG Midazolam, unter den Aspekten Anxiolyse, Analgesie, Sedierung und Amnesie eine Alternative zu Pentazocin/Midazolam ist. Kontrollgruppe (KG): Lokalanasthesie (LA) mit Articain 4%/Adrenalinzusatz 1:200.000 (n=35); Testgruppe P/M: LA und 0,40 mg/kg KG Pentazocin/0,075 mg/kg KG Midazolam i.v. (n=35); Testgruppe K25/M: LA und 0,25 mg/kg KG Ketamin/0,075 mg/kg KG Midazolam i.v. (n=35); Testgruppe K50/M: LA und 0,50 mg/kg KG Ketamin/0,075 mg/kg KG Midazolam i.v. (n=35). Die LA wurde 3 min nac…