1443124-69-3Relevant articles and documents
γ-Aminobutyric acid(C) (GABAC) selective antagonists derived from the bioisosteric modification of 4-aminocyclopent-1-enecarboxylic acid: Amides and hydroxamates
Locock, Katherine E. S.,Yamamoto, Izumi,Tran, Priscilla,Hanrahan, Jane R.,Chebib, Mary,Johnston, Graham A. R.,Allan, Robin D.
, p. 5626 - 5630 (2013)
Series of compounds were generated via the bioisosteric replacement of the carboxylate of 4-ACPCA (2) with hydroxamate or amide groups. All compounds from this study exhibited increased selectivity for GABAC, the most potent being 4-ACPHA (10a, IC50 = 13 μM) and 4-ACPAM (11a, IC 50 = 10 μM). This provides evidence that a zwitterionic structure is not essential for GABAC antagonists, rather the emphasis lies in appropriate heteroatoms to participate in hydrogen bonding.