Yasumichi Fukuda

Summary

Publications

  1. Singh S, Kaelin D, Wu J, Miesel L, Tan C, Gill C, et al. Hydroxy tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of RHS moiety (Part-3). Bioorg Med Chem Lett. 2015;25:2473-8 pubmed publisher
    ..Bicyclic heterocycles appeared to be the best RHS moiety for the hydroxy-tricyclic oxabicyclooctane linked NBTIs. ..
  2. Singh S, Kaelin D, Wu J, Miesel L, Tan C, Meinke P, et al. Structure activity relationship of pyridoxazinone substituted RHS analogs of oxabicyclooctane-linked 1,5-naphthyridinyl novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-6). Bioorg Med Chem Lett. 2015;25:3636-43 pubmed publisher
    ..This would suggest likely an altered binding mode of the linker position-7,8 amide containing compounds. The amides showed highly improved hERG (functional IC50 >30 μM) profile. ..
  3. Singh S, Kaelin D, Meinke P, Wu J, Miesel L, Tan C, et al. Structure activity relationship of C-2 ether substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-5). Bioorg Med Chem Lett. 2015;25:3630-5 pubmed publisher
    ..One of the best compounds was hydroxy propyl ether (16), which mainly retained the potency, spectrum and in vivo efficacy of AM8085 associated with the decreased hERG activity and improved physical property. ..
  4. Singh S, Kaelin D, Wu J, Miesel L, Tan C, Black T, et al. Tricyclic 1,5-naphthyridinone oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents-SAR of left-hand-side moiety (Part-2). Bioorg Med Chem Lett. 2015;25:1831-5 pubmed publisher
    ..The discovery, synthesis, SAR and X-ray crystal structure of the left-hand-side tricyclic 1,5-naphthyridinone based oxabicyclooctane linked NBTIs are described. ..
  5. Singh S, Kaelin D, Wu J, Miesel L, Tan C, Meinke P, et al. Structure activity relationship of substituted 1,5-naphthyridine analogs of oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad-spectrum antibacterial agents (Part-4). Bioorg Med Chem Lett. 2015;25:2409-15 pubmed publisher
    ..Substitutions on the other three carbons generally have detrimental effect on the activity. No clear hERG activity SAR emerged from these substitutions. ..

Collaborators