Bioorganic & medicinal chemistry letters

Design, synthesis, and bioactivity of novel inhibitors of E. coli aspartate transcarbamoylase

J Eldo, S Heng, ER Kantrowitz

Index: Eldo, Joby; Heng, Sabrina; Kantrowitz, Evan R. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 7 p. 2086 - 2090

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Citation Number: 8

Abstract

A series of inhibitors of the aspartate transcarbamoylase, an enzyme involved in pyrimidine nucleotide biosynthesis, has been synthesized. These inhibitors are analogues of a highly potent inhibitor of this enzyme, N-phosphonacetyl-l-aspartate (PALA). Analogues have been synthesized with modifications at the α-and β-carboxylates as well as at the aspartate moiety. The ability of these compounds to inhibit the enzyme was evaluated. These ...