Novel γ-Aminobutyric Acid ρ<sub>1</sub> Receptor Antagonists; Synthesis, Pharmacological Activity and Structure−Activity Relationships

γ-Aminobutyric acid (GABA) analogues based on 4-amino-cyclopent-1-enyl phosphinic acid (34−42) and 3-aminocyclobutane phosphinic acids (51, 52, 56, 57) were investigated in order to obtain selective homomeric ρ1 GABAC receptor antagonists. The effect of the stereochemistry and phosphinic acid substituent of these compounds on potency and selectivity within the GABA receptor subtypes was investigated. Compounds of high potency at GABAC ρ1 receptors (36, KB = 0.78 μM) and selectivity greater than 100 times (41, KB = 4.97 μM) were obtained. The data obtained was analyzed along with the known set of GABAC ρ1 receptor−ligands, leading to the development of a pharmacophore model for this receptor, which can be used for in silico screening.

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PID https://www.doi.org/10.1021/jm7015842.s001
URL https://figshare.com/articles/journal_contribution/Novel_Aminobutyric_Acid_sub_1_sub_Receptor_Antagonists_Synthesis_Pharmacological_Activity_and_Structure_Activity_Relationships/2928388
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Access Right Open Access
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Author Kumar, Rohan J.
Author Chebib, Mary
Author Hibbs, David E.
Author Kim, Hye-Lim
Author Johnston, Graham A. R.
Author Salam, Noeris K.
Author Hanrahan, Jane R.
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Collected From figshare
Hosted By figshare
Publication Date 2016-02-27
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Language English
Resource Type Other literature type
keyword 0.78 μ M
keyword ρ1 Receptor Antagonists
keyword 4.97 μ M
keyword homomeric ρ1 GABAC receptor antagonists
system:type publication
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Source https://science-innovation-policy.openaire.eu/search/publication?articleId=r37980778c78::40c0a1dcfd67c2e0f492ccc336af43c5
Author jsonws_user
Last Updated 26 December 2020, 19:48 (CET)
Created 26 December 2020, 19:48 (CET)