- D1 agonist and/or D2 antagonist dopamine receptor properties of a series of ergoline derivatives: A structure-activity study
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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.
- Mantegani, Sergio,Arlandini, Emanuele,Bandiera, Tiziano,Borghi, Daniela,Brambilla, Enzo,Caccia, Carla,Cervini, Maria Antonietta,Cremonesi, Paolo,McArthur, Robert Albert,Traquandi, Gabriella,Varasi, Mario
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p. 107 - 124
(2007/10/03)
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- 3-oxo-piperazin-1-yl-ergolines exhibiting antidopaminergic activity
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The invention relates to ergoline derivatives having the general formula (I): STR1 where R=H, CH3 ; R1 =H, halogen, CH3, phenylthio, C1 -C4 alkylthio; R2 =H, CH3 O, and R3 =H or R2 +R3 =chemical bond; R4 =C1 -C4 hydrocarbon; R5, R6, R8, R9 independently=H, C1 -C4 alkyl, or R5, R8 independently=H, C1 -C4 alkyl and R6 +R9 =CH2 CH2, CH2 CH2 CH2 ; R7 =H, C1 -C4 alkyl, phenyl, NR'R"; R',R" independently=H, C1 -C4 alkyl, acyl or NR'R"=heterocyclic ring; W=0, H2 ; n=0, 1, 2, and their pharmaceutically acceptable salts, these compounds exhibiting antihypertensive activity making them useful anxiolytic and antipsychotic agents. A process for their preparation and pharmaceutical compositions containing them are also described.
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