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Design and Synthesis of D[sub.3]R Bitopic Ligands with Flexible Secondary Binding Fragments: Radioligand Binding and Computational Chemistry Studies

Molecules (Basel, Switzerland), 2023-12, Vol.29 (1) [Peer Reviewed Journal]

COPYRIGHT 2023 MDPI AG ;ISSN: 1420-3049 ;EISSN: 1420-3049 ;DOI: 10.3390/molecules29010123

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  • Title:
    Design and Synthesis of D[sub.3]R Bitopic Ligands with Flexible Secondary Binding Fragments: Radioligand Binding and Computational Chemistry Studies
  • Author: Tian, Gui-Long ; Hsieh, Chia-Ju ; Taylor, Michelle ; Lee, Ji Youn ; Luedtke, Robert R ; Mach, Robert H
  • Subjects: Antiparkinsonian agents ; Dopamine receptors ; Nervous system diseases ; Schizophrenia
  • Is Part Of: Molecules (Basel, Switzerland), 2023-12, Vol.29 (1)
  • Description: A series of bitopic ligands based on Fallypride with a flexible secondary binding fragment (SBF) were prepared with the goal of preparing a D[sub.3]R-selective compound. The effect of the flexible linker ((R,S)-trans-2a–d), SBFs ((R,S)-trans-2h–j), and the chirality of orthosteric binding fragments (OBFs) ((S,R)-trans-d, (S,R)-trans-i, (S,S)-trans-d, (S,S)-trans-i, (R,R)-trans-d, and (R,R)-trans-i) were evaluated in in vitro binding assays. Computational chemistry studies revealed that the interaction of the fragment binding to the SBF increased the distance between the pyrrolidine nitrogen and ASP110[sup.3.32] of the D[sub.3]R, thereby reducing the D[sub.3]R affinity to a suboptimal level.
  • Publisher: MDPI AG
  • Language: English
  • Identifier: ISSN: 1420-3049
    EISSN: 1420-3049
    DOI: 10.3390/molecules29010123
  • Source: Geneva Foundation Free Medical Journals at publisher websites
    PubMed Central
    Alma/SFX Local Collection
    ProQuest Central
    DOAJ Directory of Open Access Journals
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