Author/Authors :
Edward W. Brooke، نويسنده , , Stephen G. Davies، نويسنده , , Andrew W. Mulvaney، نويسنده , , Minoru Okada، نويسنده , , Frédérique Pompeo، نويسنده , , Edith Sim، نويسنده , , Richard J. Vickers، نويسنده , , Isaac M. Westwood، نويسنده ,
Abstract :
The synthesis and inhibitory activity of a series of 5-substituted-(1,1-dioxo-2,3-dihydro-1H-1λ6-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.