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Updated: Sep 30, 2026

Structure-Guided Design and Development of Novel Cyclophilin A Inhibitors and Ganoderiol-F Derivatives: An In-Silico Approach
Published on: June 23, 2026
Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the
Durk Dijkstra1, Nienke Rodenhuis, Erik S Vermeulen
1Department of Medicinal Chemistry, University of Groningen, Antonius Deusinglaan 1, NL-9713 AV Groningen, The Netherlands. D.Dijkstra@farm.rug.nl
Abstract:
The present study describes the synthesis and in vitro pharmacology of a novel series of dopaminergic agents in which the classical phenylethylamine pharmacophore is replaced by a thienylethylamine moiety. In general, the novel compounds showed a moderate affinity for the dopamine (DA) D(2) and D(3) receptors. When the thienylethylamine moiety is fixed in a rigid system, the affinity for the DA receptor is significantly increased. However, in the tricyclic hexahydrothianaphthoxazine structure, the affinity for the DA receptors is diminished.
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