Search results for "Sulfonyl"
showing 10 items of 210 documents
Über die Darstellung und Polymerisation von 4-Vinyldiphenyl, 11-Vinyl-p-terphenyl und 1 2-Vinyl-p-terphenyl
1969
Fur die Darstellung von 4-Vinyldiphenyl und 11-Vinyl-p-terphenyl wurden einfache, verallgemeinerungsfahige Synthesen ausgearbeitet. Durch Umsetzung entsprechender Carbinole mit Methansulfonsaurechlorid in Pyridin gelang die Darstellung der Vinylverbindungen in einer einstufigen Reaktion. Die Untersuchung der radikalischen Copolymerization der Monomeren mit Styrol ergab bei 4-Vinyldiphenyl und 12-Vinyl-p-terphenyl einen bevorzugten Einbau in die Polymerketten, wahrend 11-Vinyl-p-terphenyl nur in untergeordnetem Mase in Polystyrolketten eingebaut wurde. The synthesis of 4-vinylbiphenyl and 11-vinyl-p-terphenyl was performed by a simple synthetic route. By reaction of the corresponding alcohol…
Calix[4]arenes bridged at the lower rim
1990
Calix[41 arenes, in which two opposite p-positions are linked by an aliphatic chain, and their derivatives show transport or complexation properties strongly dependent on the length of this chain. Bicyclo-calix[4]arenes, a special case of 1,3-bridged calix[41 arenes, and annelated calix[41 arenes, a special case of 1 ,&bridged calix [4] arenes, are also described. Although the preferred conformation of calix[4]arenes is the coneconformation due to its stabilization by a cyclic array of hydrogen bonds between the phenolic hydroxyl goups, these molecules are flexible, with a cone to cone inversion rate of about 150 8-1 for a calix[glarene at 47OC (ref. 1). The cone (or any other) conformation…
Crystal structure and Hirshfeld surface analysis of 1-(2,4-dichlorobenzyl)-5-methyl-N-(thiophene-2-sulfonyl)-1H-pyrazole-3-carboxamide
2018
In the title compound, C16H13Cl2N3O3S2, the thiophene ring is disordered in a 0.762 (3):0.238 (3) ratio by an approximate 180° rotation of the ring around the S—C bond linking the ring to the sulfonyl unit. The dichlorobenzene group is also disordered over two sets of sites with the same occupancy ratio. The molecular conformation is stabilized by intramolecular C—H...Cl and C—H...N hydrogen bonds, forming rings with graph-set notation S(5). In the crystal, pairs of molecules are linked by N—H...O and C—H...O hydrogen bonds, forming inversion dimers with graph-set notation R 2 2(8) and R 1 2(11), which are connected by C—H...O hydrogen-bonding interactions into ribbons parallel to (100). Th…
Crystal structure of (2R*,3aR*)-2-phenylsulfonyl-2,3,3a,4,5,6-hexahydropyrrolo[1,2-b]isoxazole
2017
The title compound, C12H15NO3S, was prepared by 1,3-dipolar cycloaddition of 3,4-dihydro-2H-pyrrole 1-oxide and phenyl vinyl sulfone. In the molecule, both fused five-membered rings display a twisted conformation. In the crystal, C—H...O hydrogen bonds link neighbouring molecules, forming chains running parallel to thebaxis.
Effects of sulphonylureas on spontaneous motility and induced contractions in rat isolated uterus
1986
Abstract To clarify the action of sulphonylureas on calcium, the effect of tolbutamide and ghbenclamide has been investigated on a Ca-dependent process, the contractile activity of uterine smooth muscle. Both sulphonylureas antagonized the contractions evoked by CaCl2 in a non-competitive manner when the uterus was maintained in depolarizing solution and did not affect the spontaneous contractions of rat uterus. The capacity of tolbutamide and ghbenclamide to relax vanadate-induced contraction of rat uterus in Ca-free medium suggests that sulphonylureas may have an intracellular site of action related to cytosolic free Ca levels, or effect a reduction in Ca action.
Analysis of Rabbit Vascular Responses to DBI, an Ingol Derivative Isolated from Euphorbia canariensis
1997
Abstract We have analysed the effects of 7,12-O-diacetyl-8-O-benzoil-2,3-diepiingol (DBI), an ingol derivative isolated from E. canariensis, on isometric tension developed by isolated rabbit basilar and carotid arteries. Concentration-response curves to DBI (10−8 - 3 × 10−5 m) were obtained cumulatively in both arteries at resting tension and active tone (KC1, 50 mm). At resting tension, DBI induced a concentration-dependent contraction, which was not inhibited in Ca2+-free medium. H7 (1-(5-isoquinoline sulphonyl)-2-methylpiperazine dichloride) (10−4 m) inhibited the DBI-induced contraction both in basilar and in carotid arteries. Calmidazolium (10−4 m) inhibited the maximum contraction of …
A Decision Support Tool for Appropriate Glucose-Lowering Therapy in Patients with Type 2 Diabetes
2015
Contains fulltext : 152084.pdf (Publisher’s version ) (Open Access) BACKGROUND: Optimal glucose-lowering therapy in type 2 diabetes mellitus requires a patient-specific approach. Although a good framework, current guidelines are insufficiently detailed to address the different phenotypes and individual needs of patients seen in daily practice. We developed a patient-specific decision support tool based on a systematic analysis of expert opinion. MATERIALS AND METHODS: Based on the American Diabetes Association (ADA)/European Association for the Study of Diabetes (EASD) 2012 position statement, a panel of 12 European experts rated the appropriateness (RAND/UCLA Appropriateness Method) of tre…
Inhibition of intracellular Ca2+ release by a Rho-kinase inhibitor for the treatment of ischemic damage in primary cultured rat hippocampal neurons.
2008
The effects of hydroxy fasudil, a specific Rho-kinase inhibitor, on behavior and brain neuronal activity in animal studies have been described previously. However, whether a Rho-kinase inhibitor can directly protect neurons against ischemic damage and the molecular mechanisms underlying these effects are poorly understood. The present work was designed to investigate the effect of hydroxy fasudil against oxygen-glucose deprivation (OGD) induced acute neuronal injury and the underlying mechanisms in vitro. Pretreatment with hydroxy fasudil at 5 and 10 microM could concentration-dependently improve cell viability and decrease Lactate dehydrogenase (LDH) level in extracellular solution of neur…
Synthesis and in vitro evaluation of (S)-2-([11C]methoxy)-4-[3-methyl-1-(2-piperidine-1-yl-phenyl)-butyl-carbamoyl]-benzoic acid ([11C]methoxy-repagl…
2004
The 11 C-labeled sulfonylurea receptor 1 (SUR1) ligand (S)-2-(( 11 C)methoxy)-4-(3-methyl-1-(2-piperidine-1-yl-phenyl)- butyl-carbamoyl)-benzoic acid (( 11 C)methoxy-repaglinide) was synthesized in an overall radiochemical yield of 35% after 55 min with a radiochemical purity higher than 99%. This compound is considered for the noninvasive investigation of the SUR1 receptor status of pancreatic b-cells by positron emission tomography (PET) in the context of type 1 and type 2 diabetes. The specific activity was 40-70 GBq/lmol. In vitro testing of the nonradioactive methoxy-repaglinide was performed to characterize the affinity for binding to the human SUR1 isoform. Methoxy-repaglinide induce…
(2-Pyridyl)sulfonyl Groups for ortho -Directing Palladium- Catalyzed Carbon-Halogen Bond Formation at Functionalized Arenes
2017
International audience; We describe an efficient palladium-catalyzed selective C-H ortho-monohalogenation (X=I, Br, Cl, F) of various functionalized (2-pyridyl) aryl-sulfones. ortho-, meta-and para-functionalization is tolerated at the arene group which undergoes C-H halogenation. Some modifications are also possible on the 2-(arylsulfonyl) heteroaryl directing groups. A comparison of the halogenation efficiency suggests that bromination is the practical method of choice, while chlorination and fluorination are possible but more challenging. Under forcing conditions ortho-dihalogenation can also be achieved.