92765-39-4Relevant academic research and scientific papers
Synthesis of Oxorhenium(V) and Oxotechnetium(V) Complexes That Bind to Amyloid-β Plaques
Hayne, David J.,White, Jonathan M.,McLean, Catriona A.,Villemagne, Victor L.,Barnham, Kevin J.,Donnelly, Paul S.
, p. 7944 - 7953 (2016)
Alzheimer's disease is characterized by the presence of amyloid plaques in the brain. The primary constituents of the plaques are aggregated forms of the amyloid-β (Aβ) peptide. With the goal of preparing technetium-99m complexes that bind to Aβ plaques with the potential to be diagnostic imaging agents for Alzheimer's disease, new tetradentate ligands capable of forming neutral and lipophilic complexes with oxotechentium(V) and oxorhenium(V) were prepared. Nonradioactive isotopes of technetium are not available so rhenium was used as a surrogate for exploratory chemistry. Two planar tetradentate N3O ligands were prepared that form charge-neutral complexes with oxorhenium(v) as well as a ligand featuring a styrylpyridyl functional group designed to bind to Aβ plaques. All three ligands formed complexes with oxorhenium(V), and each complex was characterized by NMR spectroscopy, mass spectrometry, and X-ray crystallography. The oxorhenium(V) complex with a styrylpyridyl functional group binds to Aβ plaques present in post-mortem human brain tissue. The chemistry was extrapolated to technetium-99m at the tracer level for two of the ligands. The resulting oxotechnetium(V) complexes were sufficiently lipophilic and charge-neutral to suggest that they have the potential to cross the blood-brain barrier but exhibited modest stability with respect to exchange with histidine. The chemistry presented here identifies a strategy to integrate styrylpyridyl functional groups into tetradentate ligands capable of forming complexes with [M=O]3+ cores (M = Re or Tc).
Synthesis and Characterization of Fatty Acid Conjugates of Niacin and Salicylic Acid
Vu, Chi B.,Bemis, Jean E.,Benson, Ericka,Bista, Pradeep,Carney, David,Fahrner, Richard,Lee, Diana,Liu, Feng,Lonkar, Pallavi,Milne, Jill C.,Nichols, Andrew J.,Picarella, Dominic,Shoelson, Adam,Smith, Jesse,Ting, Amal,Wensley, Allison,Yeager, Maisy,Zimmer, Michael,Jirousek, Michael R.
, p. 1217 - 1231 (2016/02/23)
This report describes the synthesis and preliminary biological characterization of novel fatty acid niacin conjugates and fatty acid salicylate conjugates. These molecular entities were created by covalently linking two bioactive molecules, either niacin
PHENOXYPROPANOL DERIVATIVES AND THEIR USE IN TREATING CARDIAC AND CARDIOVASCULAR DISEASES
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Page/Page column 31, (2012/02/01)
A compound of formula I-0, and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein Z1 is C1-C4 linear or branched alkyl or alkenyl; R4 is selected from unsubstituted and substituted C3-C8 cycloalkyl, C1-C8 linear or branched alkyl, C2-5 alkenyl, C6-C10 heteroaryl or aryl, or C3-C8 heterocyclyl which may be part unsaturated, and combinations thereof; is linear C2-3 alkylene,; X1 is selected from NH and O; X2 is selected from unsaturated C and unsaturated S; and X3 is selected from NH and CH2; or one of X1 and X3 is a single bond; or X1 is O and X2 and X3 together are a single bond; and R7 is selected from oxo, F, Cl, Br, CN, NH2, NR92, NO2, CF3, OR9, COR9, OCOR9, COOR9, NR9COR9, CONR92 SO2NR92, NR9SO2R9; and R8 is selected from C1-5 alkyl, C1-5 alkoxyl, C2-5 alkenyl or alkynyl, C6-10) aryl and C3-8 cycloalkyl and combinations thereof, which may be unsubstituted or f urther substituted by one or more F, Cl, Br, CN, NH2, NR32, NO2, CF3; and R9 is selected from H and a group R8 as hereinbefore defined; n7 and n8 and the sum thereof are independently selected from zero and the whole number integer 1 to 4; processes for the preparation thereof, compositions and uses.
LIPOIC ACID ACYLATED SALICYLATE DERIVATIVES AND THEIR USES
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Page/Page column 28, (2011/04/24)
The invention relates to lipoic acid acylated salicylate derivatives; compositions comprising an effective amount of a lipoic acid acylated salicylate derivative; and methods for treating or preventing an metabolic disease comprising the administration of
A convenient synthesis of nickel(II) and cobalt(II) complexes of unsymmetrical salen-type ligands and their application as catalysts for the oxidation of 2,6-dimethylphenol and 1,5-dihydroxynaphthalene by molecular oxygen
Adam, Waldemar,Saha-Moeller, Chantu R.,Ganeshpure, Pralhad A.
, p. 56 - 62 (2007/10/03)
Salen-type ligands 1-4 have been synthesized in high yields, from which the nickel(II) complexes 9-11 and the cobalt(II) complexes 12 and 13 have been prepared and characterized. The complexes have been assessed for their ability to activate molecular oxygen in the catalytic oxidation of phenols, namely, 2,6-dimethylphenol and 1,5-dihydroxynaphthalene. The nickel complexes 9-11 are inactive in the oxidation of the phenols but the cobalt complexes 12 and 13 show high catalytic activity.
