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

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.
Publication status:
Published

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Authors


Brooke, EW More by this author
More by this author
Institution:
University of Oxford
Department:
Oxford, MPLS, Chemistry, Organic Chemistry
Mulvaney, AW More by this author
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Journal:
Bioorganic and medicinal chemistry letters
Volume:
13
Issue:
15
Pages:
2527-2530
Publication date:
2003-08-05
DOI:
EISSN:
1464-3405
ISSN:
0960-894X
URN:
uuid:40d1846f-a631-4b81-bc19-841b2e13c19a
Source identifiers:
110534
Local pid:
pubs:110534

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