Structure–activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors
DOI: 10.1016/j.bmcl.2006.12.005
Title: Structure–activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors
Journal Title: Bioorganic & Medicinal Chemistry Letters
Volume: 17
Issue: 5
Publication Date: 1 March 2007
Start Page: 1312
End Page: 1320
Published online: online 15 December 2006
ISSN: 0960-894X
Affiliations:

  • a Department of Chemistry, Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA

  • b Department of Antibacterial Pharmacology, Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA

  • c NAEJA Pharmaceuticals, 4290-91A Street, Edmonton, Alta., Canada T6E5V2
  • Abstract: of 3-aminoquinazolinediones was synthesized and evaluated for its antibacterial and DNA gyrase activity. The SAR around the quinazolinedione core was explored and the optimal substitutions were combined to give two compounds, 2r and 2s, with exceptional enzyme potency (IC50 =  0.2 μM) and activity against Gram-positive organisms (MIC’s  =  0.015–0.06 μ g/mL).
    Accepted: 1 December 2006
    Received: 31 October 2006
    Keywords: 3-Aminoquinazolinediones; Antibacterial agents; DNA gyrase inhibitors; Topoisomerase inhibitors; Antibacterial activity
    Tel: +1 734 622 5496
    Fax: +1 734 622 2265
    Email: tuan.tran@pfizer.com

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