European Journal of Medicinal Chemistry p. 107 - 124 (1999)
Update date:2022-07-29
Topics:
Mantegani, Sergio
Arlandini, Emanuele
Bandiera, Tiziano
Borghi, Daniela
Brambilla, Enzo
Caccia, Carla
Cervini, Maria Antonietta
Cremonesi, Paolo
McArthur, Robert Albert
Traquandi, Gabriella
Varasi, Mario
A series of (3,5-dioxopiperazin-1-yl)ergoline derivatives has been synthesised and evaluated in vitro and in vivo for their dopaminergic D1 and D2 components. The structural contributions to the pharmacological profile of the ergoline skeleton, its substituents on positions 1, 2, 6, 9, and the 3,5-dioxopiperazin-1-yl portion of the molecule were examined. Structure- activity relationships within this series suggested that substitution on the ergoline skeleton in position 1 or 2 and on the 3,5-dioxopiperazin-4-nitrogen generated compounds with a spectrum of dopamine agonistic/antagonistic activity sensitive to both the nature and position of substituents.
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