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 ergolines 2 have modest prolactin-inhibiting and rat antimuricidal activities and possess significant alpha-blocking and antiserotonin properties.
D000374:Aggression / Q000187:drug effects; D000818:Animals; D004873:Ergolines / Q000138:chemical synthesis* / Q000494:pharmacology; D005260:Female; D006801:Humans; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects; D011388:Prolactin / Q000097:blood; D051381:Rats; D012702:Serotonin Antagonists; D014590:Uterine Contraction / Q000187:drug effects
D004873:Ergolines; D012702:Serotonin Antagonists; D011388:Prolactin