80534-78-7Relevant academic research and scientific papers
NOVEL COMPOUNDS
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Page/Page column 40; 41, (2011/07/07)
The present invention relates to novel NADPH oxidase II inhibitors and their use in the treatment of diseases mediated by the NADPH oxidase II enzyme.
Synthesis and analgesic activity of 1,3,3,4,4-substituted piperidines
Huegi,Maurer,Romer,Petcher
, p. 487 - 494 (2007/10/02)
A series of 1,3,3,4,4-substituted piperidines has been prepared by a regioselective lithium ethylacetate condensation with cis/trans 2-butenoic or 2-propenoic acid ethylester derivatives, therapy affording the propane dicarboxylic acid diethylesters which were subjected to a number of reactions to give the title compounds. Their analgesic, morphinomimetic and morphine-antagonistic properties were determined. X-ray analysis of the 4-(3-hydroxyphenyl)-piperidine confirmed the undesired equatorial phenyl conformer explaining the possible failure to show biological properties throughout the 4-methyl-4-phenyl series. Although no strong analygesia or morphine-antagonism was found in the 4,4-diphenyl-series either, some of these compounds possess binding affinities to the 3H-naloxone binding site comparable to the reference compound bremazocine and morphine. As of yet we can only speculate why compounds with a high affinity to the receptor neither show analgesia, nor antagonize morphine induced analgesia.
SYNTHESE RADICALAIRE D'ANALGESIQUES POTENTIELS: ARYL-4 PIPERIDINES SUBSTITUEES EN 2 ET BENZOMORPHANES
Stella, L.,Raynier, B.,Surzur, J. M.
, p. 2843 - 2854 (2007/10/02)
The synthesis of a series of 3-aryl 5-hexenyl amines and the cyclisations of the corresponding N-chloroamines are described.When the ring closure results from the amino radical addition to the ethylenic double bond, 2-chloromethyl 4-phenyl piperidines are obtained.These compounds lead by intramolecular Friedel-Crafts reaction to varied substituted 6,7-benzomorphanes.When the phenyl ring is substituted with a methoxyl group, the cyclisation proceeds via homolytic aromatic substitution and 4-allyl tetrahydroquinolines are formed.
