174609-82-6Relevant articles and documents
3-(piperazinylpropyl)indoles: Selective, orally bioavailable h5-HT(1D) receptor agonists as potential antimigraine agents
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.
, p. 691 - 705 (2007/10/03)
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
Piperazine, piperidine and tetrahydropyridine derivative of indol-3-alkyl as 5-HT1D-α agonists
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, (2008/06/13)
Compounds of formula (I), or a salt or prodrug thereof, wherein Z represents an optionally substituted five-membered heteroaromatic ring selected from furan, thiophene, pyrrole, oxazole, thiazole, isoxazole, isothiazole, imidazole, pyrazole, oxadiazole, thiadiazole, triazole and tetrazole; E represents a chemical bond or a straight or branched alkylene chain containing from 1 to 4 carbon atoms; Q represents a straight or branched alkylene chain containing from 1 to 6 carbon atoms, optionally substituted in any position by a hydroxy group; T represents nitrogen or CH; U represents nitrogen or C--R2 ; V represents oxygen, sulphur or N--R3 ; --F--G-- represents --CH2--N--, --CH2--CH-- or --CH=C--; R1 represents C3-6 alkenyl, C3-6 alkynyl, aryl(C1-6)alkyl or heteroaryl(C1-6)alkyl, any of which groups may be optionally substituted; and R2 and R3 independently represent hydrogen or C1-6 alkyl are selective agonists of 5-HT1D receptors, being potent agonists of the human 5-HT1Dalpha receptor subtype, while possessing at least a 10-fold selective affinity for the 5-HT1Dalpha receptor subtype, relative to the 5-HT1Dbeta 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.