Propellanes as Rigid Scaffolds for the Stereodefined Attachment of σ-Pharmacophoric Structural Elements to Achieve σ Affinity

Propellanes as Rigid Scaffolds for the Stereodefined Attachment of σ-Pharmacophoric Structural Elements to Achieve σ Affinity

Following the concept of conformationally restriction of ligands to achieve high receptor affinity, we exploited the propellane system as rigid scaffold allowing the stereodefined attachment of various substituents. Three types of ligands were designed, synthesized and pharmacologically evaluated as...

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Bibliographic Details
Main Authors: Héctor Torres-Gómez, Constantin Daniliuc, Dirk Schepmann, Erik Laurini, Sabrina Pricl, Bernhard Wünsch
Format: Article
Language:English
Published: MDPI AG 2021-05-01
Series:International Journal of Molecular Sciences
Subjects:
σ receptors
rigidity
propellanes
azapropellanes
stereochemistry
X-ray crystal structures
Online Access:https://www.mdpi.com/1422-0067/22/11/5685

Internet

https://www.mdpi.com/1422-0067/22/11/5685

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