Literature DB >> 17189694

Synthesis and biological evaluation of thiazolidine-2-one 1,1-dioxide as inhibitors of Escherichia coli beta-ketoacyl-ACP-synthase III (FabH).

Mamoun M Alhamadsheh1, Norman C Waters, Donald P Huddler, Mara Kreishman-Deitrick, Galina Florova, Kevin A Reynolds.   

Abstract

A series of cyclic sulfones has been synthesized and their activity against beta-ketoacyl-ACP-synthase III (FabH) has been investigated. The compounds are selectively active against Escherichia coli FabH (ecFabH), but not Mycobacterium tuberculosis FabH (mtFabH) or Plasmodium falciparum KASIII (PfKASIII). The activity against ecFabH ranges from 0.9 to >100microM and follows a consistent general SAR trend. Many of the compounds were shown to have antimalarial activity against chloroquine (CQ)-sensitive (D6) P. falciparum (IC(50)=5.3microM for the most potent inhibitor) and some were active against E. coli (MIC=6.6microg/ml for the most potent inhibitor).

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Year:  2006        PMID： 17189694     DOI： 10.1016/j.bmcl.2006.11.067

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


  6 in total

Review 1.  Antibacterial targets in fatty acid biosynthesis.

Authors:  H Tonie Wright; Kevin A Reynolds
Journal:  Curr Opin Microbiol       Date:  2007-08-17       Impact factor: 7.934

2.  Substrate recognition by β-ketoacyl-ACP synthases.

Authors:  Janine G Borgaro; Andrew Chang; Carl A Machutta; Xujie Zhang; Peter J Tonge
Journal:  Biochemistry       Date:  2011-11-17       Impact factor: 3.162

3.  Molecular dynamics and docking simulations as a proof of high flexibility in E. coli FabH and its relevance for accurate inhibitor modeling.

Authors:  Yunierkis Pérez-Castillo; Matheus Froeyen; Miguel Angel Cabrera-Pérez; Ann Nowé
Journal:  J Comput Aided Mol Des       Date:  2011-04-23       Impact factor: 3.686

Review 4.  3-Ketoacyl-ACP synthase (KAS) III homologues and their roles in natural product biosynthesis.

Authors:  Risa Nofiani; Benjamin Philmus; Yosi Nindita; Taifo Mahmud
Journal:  Medchemcomm       Date:  2019-04-29       Impact factor: 3.597

5.  Targeting the fatty acid biosynthesis enzyme, beta-ketoacyl-acyl carrier protein synthase III (PfKASIII), in the identification of novel antimalarial agents.

Authors:  Patricia J Lee; Jayendra B Bhonsle; Heather W Gaona; Donald P Huddler; Tiffany N Heady; Mara Kreishman-Deitrick; Apurba Bhattacharjee; William F McCalmont; Lucia Gerena; Miriam Lopez-Sanchez; Norma E Roncal; Thomas H Hudson; Jacob D Johnson; Sean T Prigge; Norman C Waters
Journal:  J Med Chem       Date:  2009-02-26       Impact factor: 7.446

6.  Synthesis, Antimicrobial Activity, Structure-Activity Relationship, and Molecular Docking Studies of Indole Diketopiperazine Alkaloids.

Authors:  Bin Jia; Yang-Min Ma; Bin Liu; Pu Chen; Yan Hu; Rui Zhang
Journal:  Front Chem       Date:  2019-11-29       Impact factor: 5.221
  6 in total

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