Literature DB >> 12852958

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

Edward W Brooke1, Stephen G Davies, Andrew W Mulvaney, Minoru Okada, Frédérique Pompeo, Edith Sim, Richard J Vickers, Isaac M Westwood.   

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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Year:  2003        PMID： 12852958     DOI： 10.1016/s0960-894x(03)00484-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  13 in total

1.  Expression, purification, characterization and structure of Pseudomonas aeruginosa arylamine N-acetyltransferase.

Authors:  Isaac M Westwood; Simon J Holton; Fernando Rodrigues-Lima; Jean-Marie Dupret; Sanjib Bhakta; Martin E M Noble; Edith Sim
Journal:  Biochem J       Date:  2005-01-15       Impact factor: 3.857

2.  Structure of the full-length Serratia marcescens acetyltransferase AAC(3)-Ia in complex with coenzyme A.

Authors:  Georgy Popov; Elena Evdokimova; Peter J Stogios; Alexei Savchenko
Journal:  Protein Sci       Date:  2020-01-30       Impact factor: 6.725

Review 3.  Arylamine N-acetyltransferases: a structural perspective.

Authors:  Xiaotong Zhou; Zhiguo Ma; Dong Dong; Baojian Wu
Journal:  Br J Pharmacol       Date:  2013-06       Impact factor: 8.739

4.  Binding of the anti-tubercular drug isoniazid to the arylamine N-acetyltransferase protein from Mycobacterium smegmatis.

Authors:  James Sandy; Simon Holton; Elizabeth Fullam; Edith Sim; Martin Noble
Journal:  Protein Sci       Date:  2005-03       Impact factor: 6.725

5.  Investigation of the catalytic triad of arylamine N-acetyltransferases: essential residues required for acetyl transfer to arylamines.

Authors:  James Sandy; Adeel Mushtaq; Simon J Holton; Pamela Schartau; Martin E M Noble; Edith Sim
Journal:  Biochem J       Date:  2005-08-15       Impact factor: 3.857

6.  The actinobacterium Tsukamurella paurometabola has a functionally divergent arylamine N-acetyltransferase (NAT) homolog.

Authors:  Vasiliki Garefalaki; Evanthia Kontomina; Charalambos Ioannidis; Olga Savvidou; Christina Vagena-Pantoula; Maria-Giusy Papavergi; Ioannis Olbasalis; Dionysios Patriarcheas; Konstantina C Fylaktakidou; Tamás Felföldi; Károly Márialigeti; Giannoulis Fakis; Sotiria Boukouvala
Journal:  World J Microbiol Biotechnol       Date:  2019-10-31       Impact factor: 3.312

7.  Identification of arylamine N-acetyltransferase inhibitors as an approach towards novel anti-tuberculars.

Authors:  Isaac M Westwood; Sanjib Bhakta; Angela J Russell; Elizabeth Fullam; Matthew C Anderton; Akane Kawamura; Andrew W Mulvaney; Richard J Vickers; Veemal Bhowruth; Gurdyal S Besra; Ajit Lalvani; Stephen G Davies; Edith Sim
Journal:  Protein Cell       Date:  2010-03-18       Impact factor: 14.870

8.  Synthesis of new pyrazolyl-2, 4-thiazolidinediones as antibacterial and antifungal agents.

Authors:  Deepak K Aneja; Poonam Lohan; Sanjiv Arora; Chetan Sharma; Kamal R Aneja; Om Prakash
Journal:  Org Med Chem Lett       Date:  2011-11-08

Review 9.  Arylamine N-acetyltransferases in mycobacteria.

Authors:  Edith Sim; James Sandy; Dimitrios Evangelopoulos; Elizabeth Fullam; Sanjib Bhakta; Isaac Westwood; Anna Krylova; Nathan Lack; Martin Noble
Journal:  Curr Drug Metab       Date:  2008-07       Impact factor: 3.731

10.  Prospective virtual screening with Ultrafast Shape Recognition: the identification of novel inhibitors of arylamine N-acetyltransferases.

Authors:  Pedro J Ballester; Isaac Westwood; Nicola Laurieri; Edith Sim; W Graham Richards
Journal:  J R Soc Interface       Date:  2009-07-08       Impact factor: 4.118
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