- Mechanism insights into an unexpected isomerisation reaction observed during conversion of N-benzyl piperazinones to corresponding N-benzyl thio-piperazinones
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An interesting and surprising rearrangement was observed during the reaction of 4-N-benzyl piperazinone derivatives with Lawesson's reagent as a thionating agent. Investigation into the possible mechanism responsible for these results is reported herein.
- Miserazzi, Emanuele,Spotti, Mario Alessandro,Profeta, Roberto,Spada, Simone,Nalin, Arnaldo,Moro, Elisa,Andreotti, Daniele
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experimental part
p. 448 - 452
(2011/03/18)
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- 3-(piperazinylpropyl)indoles: Selective, orally bioavailable h5-HT(1D) receptor agonists as potential antimigraine agents
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Clinically effective antimigraine drugs such as Sumatriptan have similar affinity at h5-HT(1D) and h5-HT(1B) receptors. In the search for a h5- HT(1D)-selective agonist as an antimigraine agent, a novel series of 3- (propylpiperazinyl)indoles have been sy
- Chambers, Mark S.,Street, Leslie J.,Goodacre, Simon,Hobbs, Sarah C.,Hunt, Peter,Jelley, Richard A.,Matassa, Victor G.,Reeve, Austin J.,Sternfeld, Francine,Beer, Margaret S.,Stanton, Josephine A.,Rathbone, Denise,Watt, Alan P.,MacLeod, Angus M.
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p. 691 - 705
(2007/10/03)
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- BICYCLIC HETEROARYL-ALKYLENE-(HOMO)PIPERAZINONES AND THIONE ANALOGUES THEREOF, THEIR PREPARATION, AND THEIR USE OF AS SELECTIVE AGONISTS OF 5HT1-LIKE RECEPTORS
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A class of piperazinones, homopiperazinones and thione analogues thereof, substituted at the 1-position by an optionally substituted alkenyl, alkynyl, aryl-alkyl or heteroaryl-alkyl moiety, and linked at the 4-position via an alkylene spacer to a fused bicyclic heteroaromatic moiety, typically indolyl, are selective agonists of 5-HT. sub.1-like receptors, being potent agonists of the human 5-HT 1Dα receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT 1Dα receptor subtype relative to the 5-HT 1D. beta. subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT 1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT 1D receptor agonists.
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