Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs) |
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| Authors: | Brooke Edward W Davies Stephen G Mulvaney Andrew W Okada Minoru Pompeo Frédérique Sim Edith Vickers Richard J Westwood Isaac M |
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| Affiliation: | Department of Pharmacology, University of Oxford, Mansfield Road, Oxford OX1 3QT, UK. |
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| 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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