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. 2003 Aug 4;13(15):2527-30.
doi: 10.1016/s0960-894x(03)00484-0.

Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs)

Edward W Brooke  1 , Stephen G Davies, Andrew W Mulvaney, Minoru Okada, Frédérique Pompeo, Edith Sim, Richard J Vickers, Isaac M Westwood
Affiliations

Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs)

Edward W Brooke et al. Bioorg Med Chem Lett. .

Abstract

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.

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