Synthesis and nidation inhibitory activity of a new class of ergoline derivatives

doi:10.1016/0223-5234(89)90087-1

European Journal of Medicinal Chemistry

Volume 24, Issue 4, July–August 1989, Pages 421-426

https://doi.org/10.1016/0223-5234(89)90087-1 Get rights and content

Abstract

The synthesis and the nidation inhibitory activity (indirect evidence of prolactin activity) of a new class of ergolinyl-acylureas is described. Some structure—activity relationship considerations are also reported. N-[3-(Dimethyl-amino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propenyl)ergoline-8β-carboxamide (laboratory code FCE 21336; international non-proprietary name cabergoline) was the most interesting compound of the series and is now under extensive clinical evaluation in treatment of hyperprolactinemic disorders.

Résumé

Les auteurs ont décrit la synthèse et l'activité inhibitrice de la nidation d'une nouvelle classe d'acylurées d'ergolinyle. En outre, quelques considérations concernant la corrélation entre structure et activité ont été rapportées. Le composé le plus intéressant de la série était l'N-[(diméthylamino)-3 propyl]-N-[(éthylamino)carbonyl](propényl-2)-6 ergoline-carboxamide-8β (code de laboratoire: FCE 21336, dénomination internationale commune: cabergoline) qui est soumis maintenant à une évaluation clinique approfondie.

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Original paperSynthesis and nidation inhibitory activity of a new class of ergoline derivativesSynthèse et activité inhibitrice sur la nidation d'une nouvelle classe de dérivés de l'ergoline

Abstract

Résumé

Hum. Reprod.

Pharmacol. Rev.

Arzn.-Forsch.

Helv. Chim. Acta

J. Am. Chem. Soc.

Original paper
Synthesis and nidation inhibitory activity of a new class of ergoline derivativesSynthèse et activité inhibitrice sur la nidation d'une nouvelle classe de dérivés de l'ergoline