Literature DB >> 14684293

Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors.

Adam M Gilbert1, Matthew Kirisits, Patrick Toy, David S Nunn, Amadeo Failli, Elizabeth G Dushin, Elena Novikova, Peter J Petersen, Diane Joseph-McCarthy, Iain McFadyen, Christian C Fritz.   

Abstract

D-optimal design and Projection to Latent Structures (PLS) analysis were used to optimize screening hit 5 (B. subtilis AcpS IC(50): 15 microM, B. subtilis MIC: >200 microM) into a series of 4H-oxazol-5-one, small molecule, antibacterial, AcpS inhibitors. Specifically, 15, 16 and 18 show microM or sub-microM AcpS inhibition (IC(50)s: 15: 1.1 microM, 16: 1.5 microM, 18: 0.27 microM) and moderate antibacterial activity (MICs: 12.5-50 microM) against B. subtilis, E. faecalis ATCC, E. faecalis VRE and S. pneumo+.

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Year:  2004        PMID： 14684293     DOI： 10.1016/j.bmcl.2003.10.032

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


  7 in total

Review 1.  The phosphopantetheinyl transferases: catalysis of a post-translational modification crucial for life.

Authors:  Joris Beld; Eva C Sonnenschein; Christopher R Vickery; Joseph P Noel; Michael D Burkart
Journal:  Nat Prod Rep       Date:  2014-01       Impact factor: 13.423

2.  Escherichia coli Nissle 1917 secondary metabolism: aryl polyene biosynthesis and phosphopantetheinyl transferase crosstalk.

Authors:  Courtney V Jones; Brianna G Jarboe; Haley M Majer; Amy T Ma; Joris Beld
Journal:  Appl Microbiol Biotechnol       Date:  2021-09-21       Impact factor: 4.813

Review 3.  Mining Fatty Acid Biosynthesis for New Antimicrobials.

Authors:  Christopher D Radka; Charles O Rock
Journal:  Annu Rev Microbiol       Date:  2022-06-01       Impact factor: 16.232

4.  A homogeneous resonance energy transfer assay for phosphopantetheinyl transferase.

Authors:  Timothy L Foley; Michael D Burkart
Journal:  Anal Biochem       Date:  2009-06-30       Impact factor: 3.365

5.  A strategy to discover inhibitors of Bacillus subtilis surfactin-type phosphopantetheinyl transferase.

Authors:  Adam Yasgar; Timothy L Foley; Ajit Jadhav; James Inglese; Michael D Burkart; Anton Simeonov
Journal:  Mol Biosyst       Date:  2009-10-13

6.  Structural characterization and comparison of three acyl-carrier-protein synthases from pathogenic bacteria.

Authors:  Andrei S Halavaty; Youngchang Kim; George Minasov; Ludmilla Shuvalova; Ievgeniia Dubrovska; James Winsor; Min Zhou; Olena Onopriyenko; Tatiana Skarina; Leka Papazisi; Keehwan Kwon; Scott N Peterson; Andrzej Joachimiak; Alexei Savchenko; Wayne F Anderson
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2012-09-13

7.  4-(3-Chloro-5-(trifluoromethyl)pyridin-2-yl)-N-(4-methoxypyridin-2-yl)piperazine-1-carbothioamide (ML267), a potent inhibitor of bacterial phosphopantetheinyl transferase that attenuates secondary metabolism and thwarts bacterial growth.

Authors:  Timothy L Foley; Ganesha Rai; Adam Yasgar; Thomas Daniel; Heather L Baker; Matias Attene-Ramos; Nicolas M Kosa; William Leister; Michael D Burkart; Ajit Jadhav; Anton Simeonov; David J Maloney
Journal:  J Med Chem       Date:  2014-01-22       Impact factor: 7.446
  7 in total

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