Synthesis and biological activity of 8-arylergolines

9,10-Didehydro-6-methyl-8beta-arylergolines 2, in which the carboxyl group of lysergic acid and isolysergic acid is replaced by various aryl groups, were prepared in two steps by alkylation of aromatic substrates with the tetracyclic allylic alcohol 3, followed by aromatization with MnO2. The new er...

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Veröffentlicht in:	Journal of medicinal chemistry 1977-08, Vol.20 (8), p.1105-1107
Hauptverfasser:	Bach, Nicholas J, Kornfeld, Edmund C, Dorman, Douglas E
Format:	Artikel
Sprache:	eng
Schlagworte:	Aggression - drug effects Animals Ergolines - chemical synthesis Ergolines - pharmacology Female Humans In Vitro Techniques Muscle Contraction - drug effects Muscle, Smooth - drug effects Prolactin - blood Rats Serotonin Antagonists Uterine Contraction - drug effects
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Beschreibung
Zusammenfassung:	9,10-Didehydro-6-methyl-8beta-arylergolines 2, in which the carboxyl group of lysergic acid and isolysergic acid is replaced by various aryl groups, were prepared in two steps by alkylation of aromatic substrates with the tetracyclic allylic alcohol 3, followed by aromatization with MnO2. The new ergolines 2 have modest prolactin-inhibiting and rat antimuricidal activities and possess significant alpha-blocking and antiserotonin properties.
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00218a025