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

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 inhi...

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Main Authors: Brooke, E, Davies, S, Mulvaney, A, Okada, M, Pompeo, F, Sim, E, Vickers, R, Westwood, I
Format: Journal article
Language:English
Published: 2003
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author Brooke, E
Davies, S
Mulvaney, A
Okada, M
Pompeo, F
Sim, E
Vickers, R
Westwood, I
author_facet Brooke, E
Davies, S
Mulvaney, A
Okada, M
Pompeo, F
Sim, E
Vickers, R
Westwood, I
author_sort Brooke, E
collection OXFORD
description 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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spelling oxford-uuid:40d1846f-a631-4b81-bc19-841b2e13c19a2022-03-26T14:40:03ZSynthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:40d1846f-a631-4b81-bc19-841b2e13c19aEnglishSymplectic Elements at Oxford2003Brooke, EDavies, SMulvaney, AOkada, MPompeo, FSim, EVickers, RWestwood, IThe 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.
spellingShingle Brooke, E
Davies, S
Mulvaney, A
Okada, M
Pompeo, F
Sim, E
Vickers, R
Westwood, I
Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).
title Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).
title_full Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).
title_fullStr Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).
title_full_unstemmed Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).
title_short Synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine N-acetyltransferases (NATs).
title_sort synthesis and in vitro evaluation of novel small molecule inhibitors of bacterial arylamine n acetyltransferases nats
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