- Advances toward new antidepressants with dual serotonin transporter and 5-HT1A receptor affinity within a class of 3-aminochroman derivatives. Part 2
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Novel compounds combining a 5-HT1A moiety (3-aminochroman scaffold) and a 5-HT transporter (indole analogues) linked through a common basic nitrogen via an alkyl chain attached at the 1- or 3-position of the indole were evaluated for dual affin
- Hatzenbuhler, Nicole T.,Baudy, Reinhardt,Evrard, Deborah A.,Failli, Amedeo,Harrison, Boyd L.,Lenicek, Steven,Mewshaw, Richard E.,Saab, Annmarie,Shah, Uresh,Sze, Jean,Zhang, Minsheng,Zhou, Dahui,Chlenov, Michael,Kagan, Michael,Golembieski, Jeannette,Hornby, Geoffrey,Lai, Margaret,Smith, Deborah L.,Sullivan, Kelly M.,Schechter, Lee E.,Andree, Terrance H.
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scheme or table
p. 6980 - 7004
(2009/11/30)
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- Synthesis and biological evaluation of novel compounds within a class of 3-aminochroman derivatives with dual 5-HT1A receptor and serotonin transporter affinity
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Compounds containing a 5-carbamoyl-8-fluoro-3-amino-3,4-dihydro-2H-1- benzopyran and a 3-alkylindole moiety linked through a common basic nitrogen were prepared and evaluated for 5-HT1A affinity, serotonin rat transporter affinity, and functional antagonist activity in vitro. 26a was found to be the most potent and selective compound in this series and was shown to possess neurochemical activity in vivo by producing acute and rapid increases in 5-HT in the rat frontal cortex.
- Hatzenbuhler, Nicole T.,Evrard, Deborah A.,Harrison, Boyd L.,Huryn, Donna,Inghrim, Jennifer,Kraml, Christina,Mattes, James F.,Mewshaw, Richard E.,Zhou, Dahui,Hornby, Geoffrey,Lin, Qian,Smith, Deborah L.,Sullivan, Kelly M.,Schlechter, Lee E.,Beyer, Chad E.,Andree, Terrance H.
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p. 4785 - 4789
(2007/10/03)
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- Methoxy and hydroxy derivatives of 3,4-dihydro-3-(di-n-propylamino)-2H-1-benzopyrans: New synthesis and dopaminergic activity
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The synthesis of methoxy and hydroxy derivatives of 3,4-dihydro-3-(di-n-propylamino)-2H-1-benzopyran from readily available or commercial o-hydroxybenzaldehydes is described in six steps. The enantiomers of 8-hydroxy-3,4-dihydro-3-(di-n-propyl-amino)-2H-1-benzopyran 1b have been resolved. It is shown that the compound (-)-1b is a mroe selective D-2 agonist, compared to apomorphine.
- Al Neirabeyeh,Reynaud,Podona,Ou,Perdicakis,Coudert,Guillaumet,Pichat,Gharib,Sarda
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p. 497 - 504
(2007/10/02)
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- 5-Oxy-substituted-3-aminochroman compounds, processes for their preparation, pharmaceutical compositions containing them and methods of treatment therewith
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A compound of the formula wherein R1 is a saturated or unsaturated alkyl group having 1-5 carbon atoms or a phenylalkyl group, whereby the phenyl ring may be substituted or unsubstituted and the alkyl having 1-4 carbon atoms, R2 is hydrogen or an alkyl group having 1-5 carbon atoms, or R1 and R2 together form a 5- or 6-membered ring containing 1 or 2 heteroatoms selected from N, O and S, and enantiomers and physiologically acceptable salts thereof, processes for preparation of said compounds, pharmaceutical preparations containing said compounds, use of and method of treatment of disorders in CNS by using said compounds and intermediates.
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