Synthesis and in vitro evaluation of aspartate transcarbamoylase inhibitors.
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ABSTRACT:
SUBMITTER: Coudray L
PROVIDER: S-EPMC2783949 | biostudies-literature | 2009 Nov
REPOSITORIES: biostudies-literature
Publications
Synthesis and in vitro evaluation of aspartate transcarbamoylase inhibitors.
Coudray Laëtitia L Pennebaker Anne F AF Montchamp Jean-Luc JL
Bioorganic & medicinal chemistry 20090930 22
The design, synthesis, and evaluation of a series of novel inhibitors of aspartate transcarbamoylase (ATCase) are reported. Several submicromolar phosphorus-containing inhibitors are described, but all-carboxylate compounds are inactive. Compounds were synthesized to probe the postulated cyclic transition-state of the enzyme-catalyzed reaction. In addition, the associated role of the protonation state at the phosphorus acid moiety was evaluated using phosphinic and carboxylic acids. Although non ...[more]
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