- Lipid-lowering (hetero)aromatic tetrahydro-1,4-oxazine derivatives with antioxidant and squalene synthase inhibitory activity
-
A number of newly synthesized 2-[4-(hetero)aromatic]phenyl-2-hydroxy- tetrahydro-1,4-oxazine derivatives were found to inhibit lipid peroxidation (IC50 of the most potent was 20 μM) as well as rat squalene synthase (IC50 for most between 1-10 μM). Antidyslipidemic action was demonstrated in vivo: the most active compound decreased triglycerides, total cholesterol, and LDL-cholesterol of hyperlipidemic rats by 64, 67, and 82%, respectively, at 56 μmol/kg (ip). Most of the novel compounds are more active than the structurally related and reference biphenyl-morpholine, pointing to useful structural approaches for the design of antiatherosclerotic agents.
- Kourounakis, Angeliki P.,Charitos, Christos,Rekka, Eleni A.,Kourounakis, Panos N.
-
supporting information; experimental part
p. 5861 - 5865
(2009/09/25)
-
- Polyvinylpyridine, a versatile solid phase for coordinative immobilisation of palladium precatalysts - Applications in Suzuki-Miyaura reactions
-
The immobilisation of an oxime-based palladacycle on polyvinylpyridine (PVP) resin affords a reusable, air, moisture and thermally stable palladium precatalyst which exerts high activity in Suzuki-Miyaura reactions both in batch as well as continuous-flow processes. Evidence is presented which shows that, besides serving as an anchor for the precatalyst, PVP also acts as a scavenger for Pd particles present in solution. Georg Thieme Verlag Stuttgart.
- Solodenko, Wladimir,Mennecke, Klaas,Vogt, Carla,Gruhl, Susan,Kirschning, Andreas
-
p. 1873 - 1881
(2008/01/27)
-
- Sulfonamide derivatives
-
The present invention provides certain sulfonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
- -
-
-
- Isoxazole derivatives
-
An isoxazole derivative represented by the formula: or a pharmaceutically acceptable salt thereof useful as a therapeutic drug for auto-immune diseases and inflammatory diseases.
- -
-
-
- Liquid Crystalline Polymesomorphism in Copper(II) Complexes of β-Diketones: The Effect of the Position of a Polar Substituent
-
We have shown previously that smetic phase thermal stability in copper(II) complexes of 1-(4'-decylbiphenyl-4-yl)-3-(biphenyl-4-yl)propane-1,3-diones is considerably enhanced by the introduction of polar substituents (F, Br and CF3) into the 4'-position of the lateral biphenyl unit.The preparation of a new series of complexes is described and the transition temperatures of the ligands and complexes reveal the effect on mesophase type and stability of a polar substituent at different positions in the molecule.The effects which fluoro-substituents have on the transitiontemperatures of the β-diketone ligands and the complexes are also compared with the effects produced by similar fluoro-subsitution in terphenyl systems.
- Thompson, Neil J.,Goodby, John W.,Toyne, Kenneth J.
-
-
- Formation Constants of Cyanohydrins of Substituted Acetylbiphenyls
-
The formation constants of cyanohydrins of 2'- and 3'-substituted 4-acetylbiphenyls have been determined at 30 deg C in 80percent dioxan-water (v/v).The 3'-substituted 4-acetylbiphenyls obey the Hammett equation giving a ρ-value of 0.52; 2'-substituted cyanohydrins do not obey the Hammett equation.The formation constants of 3'-substituted 4-acetylbiphenyls and their rate constants for the reduction by sodium borohydride reveal a linear relationship (r = 0.990).The influence of 2'-substituents reveals the existence of ?-electron steric effect.
- Ananthakrishnanadar, P.,Kannan, N.
-
-
- N-1-(p-Biphenylalkyl)piperazines and their use as anti-inflammatory agents
-
This invention relates to N-1(p-biphenylalkyl) piperazines, to the processes for making such compounds and to the use of such compounds as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis.
- -
-
-