Synthesis and in vitro evaluation of aspartate transcarbamoylase inhibitors.


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… (More)
DOI: 10.1016/j.bmc.2009.09.045


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