182358-82-3Relevant academic research and scientific papers
2-Acylamino-4-phenylthiazole derivatives, preparation thereof and therapeutic application thereof
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Page/Page column 24, (2008/06/13)
The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.
Poly(ε-caprolactone) macroligands with β-diketonate binding sites: Synthesis and coordination chemistry
Bender, Jessica L.,Shen, Qun-Dong,Fraser, Cassandra L.
, p. 7277 - 7285 (2007/10/03)
Dibenzoylmethane (dbm) initiators with one and two alcohol sites were used to generate dbm end-functionalized and dbm-centered poly(ε-caprolactone) macroligands (dbmPCL and dbmPCL2) with low polydispersities (~1.1). Chelation of polymeric ligands to metal ions (Eu3+, Fe3+, Ni2+ and Cu2+) produced metal-centered star polymers, which were characterized by UV-vis and fluorescence spectroscopy, as well as gel permeation chromatography.
Radiosynthesis of (±)-(2-((4-(2-[18F]fluoroethoxy)phenyl)bis(4-methoxy- phenyl) methoxy)ethylpiperidine-3-carboxylic acid: A potential GAT-3 PET ligand to study GABAergic neuro-transmission in vivo
Schirrmacher, Ralf,Hamkens, Wilhelm,Piel, Markus,Schmitt, Ulrich,Lddens, Hartmut,Hiemke, Christoph,Rsch, Frank
, p. 627 - 642 (2007/10/03)
A dysfunction of GABAergic neurotransmission is related to diseases such as epilepsy, Huntington-disease and Parkinson-syndrome. A new 18F-fluorine labelled GABA transporter ligand for the GABA-transporter subtype GAT-3 was developed which may allow the in vivo visualisation of GABAergic neurotransmission. The precursors ethyl (2-(4-hydroxyphenyl)bis (4-methoxyphenyl)-methoxy)ethyl)-piperidine-3-carboxylate and ethyl(2-((4-(2-tosylethoxy)phenyl)-bis(4-methoxyphenyl)-methoxy) ethyl)piperidine-3-carboxylate were synthesised and labelled by the use of 2-[18F]fluoroethyltosylate or [18F]fluoride. Subsequent cleavage of the ester moiety gave the final product (±)-(2-((4-(2-[18F]fluoroethoxy)phenyl)bis(4-methoxy- phenyl)methoxy)ethyl)-piperidine-3-carboxylic acid in a decay corrected yield of 33-36%. Preliminary biodistribution kinetics were determined with BALB/c mice ex vivo for brain, liver, kidney, spleen, blood and bone. (2-((4-(2-[18F]fluoroethoxy)-phenyl)bis(4-methoxyphenyl)methoxy)- ethyl) piperidine-3-carboxylic acid showed a maximum brain uptake after 1 h p.i. of about 0.3% ID/g. Copyright
