New 4-(4-methyl-phenyl)phthalazin-1(2H)-one derivatives and their effects on alpha1-receptors.
Continuing our research aimed at obtaining new compounds with high affinity and selectivity toward alpha(1)-AR, a new series of arylpiperazine derivatives was designed, synthesized, and biologically tested. The new compounds 1-17 are characterized by a phenylphthalazin-1(2H)-one fragment connected through an alkyl chain to an arylpiperazine residue. The pharmacological profile of these compounds was evaluated for their affinity and selectivity toward alpha(1)-AR, alpha(2)-AR and toward 5HT(1A) serotoninergic receptor. A discussion on the structure-activity relationship (SAR) of these compounds is also reported.
Dipartimento di Chimica e Tecnologia del Farmaco, Università degli Studi di Perugia, Via del Liceo 1, 06123 Perugia, Italy. noemi@unipg.it
Giovannella
G
Strappaghetti
Chiara
C
Brodi
Gino
G
Giannaccini
Laura
L
Betti
D010793:Phthalazines / Q000737:chemistry / Q000494:pharmacology*; D018340:Receptors, Adrenergic, alpha-1 / Q000187:drug effects*; D013329:Structure-Activity Relationship
D010793:Phthalazines; D018340:Receptors, Adrenergic, alpha-1