85817-34-1Relevant articles and documents
Discovery of novel leukotriene A4 hydrolase inhibitors based on piperidine and piperazine scaffolds
Sandanayaka, Vincent,Mamat, Bjorn,Bhagat, Nikhil,Bedell, Louis,Halldorsdottir, Gudrun,Sigthorsdottir, Heida,Andrésson, Thorkell,Kiselyov, Alex,Gurney, Mark,Singh, Jasbir
scheme or table, p. 2851 - 2854 (2010/08/06)
Novel piperidine and piperazine derivatives have been designed and tested as inhibitors of LTA4 hydrolase (LTA4H). Most potent compounds showed good potency in both enzymatic and functional human whole blood assay. Crystallography studies further confirmed observed structure-activity relationship and LTA4H binding mode for analogs from the piperidine series.
Substituted 1,4-piperazine-heteroaryl derivatives as 5-HT1D receptor agonists
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, (2008/06/13)
A class of 1,4-disubstituted piperazine derivatives, further substituted on one of the carbon atoms of the piperazine ring, are selective agonists of 5-HT1 -like receptors, being potent agonists of the human 5-HT1Dα receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT1Dα receptor subtype relative to the 5-HT1Dβ 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-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.