Ontology highlight
ABSTRACT:
SUBMITTER: Juncosa JI
PROVIDER: S-EPMC3563932 | biostudies-literature | 2013 Feb
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry 20121220 4
We have synthesized three analogues of 4-amino-5-fluorohexanoic acids as potential inactivators of γ-aminobutyric acid aminotransferase (GABA-AT), which were designed to combine the potency of their shorter chain analogue, 4-amino-5-fluoropentanoic acid (AFPA), with the greater enzyme selectivity of the antiepileptic vigabatrin (Sabril®). Unexpectedly, these compounds failed to inactivate or inhibit the enzyme, even at high concentrations. On the basis of molecular modeling studies, we propose t ...[more]