5(10→9)abeo-ergoline derivatives: Synthesis, 5-HT(1A)-receptor affinity and selectivity

Sergio Mantegani; Luca Baumer; Enzo Brambilla; Carla Caccia; Maria Gioia Fornaretto; Robert Albert McArthur; Mario Varasi

doi:10.1016/S0223-5234(98)80062-7

5(10→9)abeo-ergoline derivatives: Synthesis, 5-HT(1A)-receptor affinity and selectivity

Sergio Mantegani, Luca Baumer, Enzo Brambilla, Carla Caccia, Maria Gioia Fornaretto, Robert Albert McArthur, Mario Varasi

Istituto Europeo di Oncologia

Research output: Contribution to journal › Article › peer-review

Abstract

The synthesis and the structure-affinity relationship (S.A.F.I.R.) study for the 5-HT(1A) receptor sites of a novel series of 5(10→9)abeo-ergoline derivatives are presented. Most derivatives showed moderate to high affinity and selectivity for 5-HT(1A) receptor sites. The structure-affinity relationship pointed out the role of the substituent at position 8, and the outstanding importance of the reduction of the indole 2,3-double bond for achieving the highest 5-HT(1A) affinity and selectivity within the compounds presented.

Original language	English
Pages (from-to)	279-292
Number of pages	14
Journal	European Journal of Medicinal Chemistry
Volume	33
Issue number	4
DOIs	https://doi.org/10.1016/S0223-5234(98)80062-7
Publication status	Published - Apr 1998

Keywords

5(10→9)abeo-ergoline derivative
5-HT(1A) receptor ligand
Ergoline derivative
Serotonin
Structure-affinity relationship

ASJC Scopus subject areas

Molecular Medicine
Organic Chemistry
Drug Discovery
Pharmaceutical Science

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10.1016/S0223-5234(98)80062-7

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5(10→9)abeo-ergoline derivatives : Synthesis, 5-HT(1A)-receptor affinity and selectivity. / Mantegani, Sergio; Baumer, Luca; Brambilla, Enzo; Caccia, Carla; Fornaretto, Maria Gioia; McArthur, Robert Albert; Varasi, Mario.

In: European Journal of Medicinal Chemistry, Vol. 33, No. 4, 04.1998, p. 279-292.

Research output: Contribution to journal › Article › peer-review

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AU - Brambilla, Enzo

AU - Caccia, Carla

AU - Fornaretto, Maria Gioia

AU - McArthur, Robert Albert

AU - Varasi, Mario

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5(10→9)abeo-ergoline derivatives: Synthesis, 5-HT(1A)-receptor affinity and selectivity

Abstract

Keywords

ASJC Scopus subject areas

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