Synthesis of potential inhibitors of the enzyme aspartate transcarbamoylase

Article abstract of DOI:10.1016/S0040-4039(00)98077-8

Two difluoromethylenephosphonates, 7 and 8, and the phosphinylmethylenephosphonate 9 were prepared as potential inhibitors of aspartate transcarbamoylase (ATCase). The synthesis of compound 8 was facilitated by development of a new direct method for converting nitroalkanes to alkanoic acids. Of the three phosphonates, the amid 7 proved to be a good inhibitor of mung bean ATCase (I₅₀ - 5 μM).