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The synthesis and inhibitory activity of a series of 5-substituted-(1,1-dioxo-2,3-dihydro-1H-1 lambda(6)-benzo[e][1,2]thiazin-4-ylidene)-thiazolidine-2,4-dione derivatives as competitive inhibitors of recombinant bacterial arylamine-N-acetyltransferases (NATs) are described. The most potent NAT inhibitors are those that contain planar hydrophobic substituents on the sultam nitrogen.

Original publication

DOI

10.1016/s0960-894x(03)00484-0

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

04/08/2003

Volume

13

Pages

2527 - 2530

Keywords

Alkylation, Arylamine N-Acetyltransferase, Bacteria, Enzyme Inhibitors, Indicators and Reagents, Kinetics, Models, Molecular, Molecular Conformation, Mycobacterium smegmatis, Salmonella typhimurium, Structure-Activity Relationship