Literature DB >> 19682901

Spiro-naphthyridinone piperidines as inhibitors of S. aureus and E. coli enoyl-ACP reductase (FabI).

Peter B Sampson1, Christine Picard, Sean Handerson, Teresa E McGrath, Megan Domagala, Andrew Leeson, Vladimir Romanov, Donald E Awrey, Dhushy Thambipillai, Elias Bardouniotis, Nachum Kaplan, Judd M Berman, Henry W Pauls.   

Abstract

Spiropiperidine naphthyridinone inhibitors of Staphylococcus aureus and Escherichia coli FabI have been prepared. Compounds 14a and 14c were identified as having sub-nanomolar E. coli FabI activity and are among the most potent FabI inhibitors yet described. The structural model of 14a bound to E. coli FabI is shown.

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Year:  2009        PMID： 19682901     DOI： 10.1016/j.bmcl.2009.07.129

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


  7 in total

Review 1.  Investigational antimicrobial agents of 2013.

Authors:  Michael J Pucci; Karen Bush
Journal:  Clin Microbiol Rev       Date:  2013-10       Impact factor: 26.132

2.  Recent Advances in the Rational Design and Optimization of Antibacterial Agents.

Authors:  Jesse A Jones; Kristopher G Virga; Giuseppe Gumina; Kirk E Hevener
Journal:  Medchemcomm       Date:  2016-07-07       Impact factor: 3.597

3.  The MUT056399 inhibitor of FabI is a new antistaphylococcal compound.

Authors:  S Escaich; L Prouvensier; M Saccomani; L Durant; M Oxoby; V Gerusz; F Moreau; V Vongsouthi; Kirsty Maher; Ian Morrissey; C Soulama-Mouze
Journal:  Antimicrob Agents Chemother       Date:  2011-08-08       Impact factor: 5.191

4.  Benzimidazole-Based FabI Inhibitors: A Promising Novel Scaffold for Anti-staphylococcal Drug Development.

Authors:  Tina L Mistry; Lena Truong; Arun K Ghosh; Michael E Johnson; Shahila Mehboob
Journal:  ACS Infect Dis       Date:  2016-10-27       Impact factor: 5.084

5.  Mode of action, in vitro activity, and in vivo efficacy of AFN-1252, a selective antistaphylococcal FabI inhibitor.

Authors:  Nachum Kaplan; Monique Albert; Donald Awrey; Elias Bardouniotis; Judd Berman; Teresa Clarke; Mandy Dorsey; Barry Hafkin; Jaillal Ramnauth; Vladimir Romanov; Molly B Schmid; Rosanne Thalakada; Jeremy Yethon; Henry W Pauls
Journal:  Antimicrob Agents Chemother       Date:  2012-09-04       Impact factor: 5.191

6.  Enhancement of Antibiotic Activity by 1,8-Naphthyridine Derivatives against Multi-Resistant Bacterial Strains.

Authors:  José B de Araújo-Neto; Maria M C da Silva; Cícera D de M Oliveira-Tintino; Iêda M Begnini; Ricardo A Rebelo; Luiz E da Silva; Sandro L Mireski; Michele C Nasato; Maria I L Krautler; Jaime Ribeiro-Filho; Abolghasem Siyadatpanah; Polrat Wilairatana; Henrique D M Coutinho; Saulo R Tintino
Journal:  Molecules       Date:  2021-12-06       Impact factor: 4.411

7.  Pharmacophore and molecular docking guided 3D-QSAR study of bacterial enoyl-ACP reductase (FabI) Inhibitors.

Authors:  Xiaoyun Lu; Man Lv; Kun Huang; Ke Ding; Qidong You
Journal:  Int J Mol Sci       Date:  2012-03-20       Impact factor: 6.208
  7 in total

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