Secondary metabolites, 3D strcuture: Trivial name – Warfarin metabolite 1

Date: 26 November 2013

Secondary metabolites, 3D strcuture: Trivial name – Warfarin metabolite 1

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Species: A. nigerSystematic name: 1,2,5-Hexanetrione, 1-(2-hydroxyphenyl)-3-phenyl-Molecular formulae: C18H16O4Molecular weight: 296Chemical abstracts number: 119465-33-7Selected references: Microbial models of mammalian metabolism: production of novel a-diketone metabolites of warfarin and phenprocoumon by Aspergillus niger. Rizzo, Jinee D.; Davis, P. J. Coll. Pharm., Univ. Texas, Austin, TX, USA. Xenobiotica (1988), 18(12), 1425-37.

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  • Title


  • Isolate from environmental sample

    A. clavatus, A. clavatus, A. clavatus

  • Patients has history of ABPA complicating long standing asthma. His total IgE has fluctuated between 2,200 and 4,600 KU/L, his Aspergillus IgE between 36.3 and 65.4 kAU/L and Aspergillus IgG from 87-154 mg/L. He has been taking long term itraconazole.

    December 2012, May 2012, AW CT Dec 2012 2, February 2010

  • Patient with chronic productive cough, chest pain and ABPA, unable to take itraconazole or nebulised amphotericin B. Smokes at least 40 roll up cigarettes a day.

    Nicotine stained fingers - image 1, Nicotine stained fingers - image 2

  • The chemical structure of the novel arylamidine T-2307


  • Laryngeal aspergillosis, probably related to inhaled corticosteroids.

    Image A., Image B., Image C., Image D.

  • VL-2397 (formerly known as ASP2397) is a novel antifungal drug initially developed by our partner, Astellas Pharma. This drug was isolated from a leaf litter fungus Acremonium species collected in a Malaysian national park. Astellas presented two posters at the 2014 ICAAC meeting which described the in vitro and the in vivo antifungal activities of this drug. The differentiating attributes from the preclinical data of VL-2397 include:

    • A novel mechanism of action, with a potential to be complementary or synergistic with the existing classes of antifungals.
    • Rapid fungal cell kill activity demonstrated in preclinical models, which was faster than marketed antifungals.
    • Activity against azole-resistant fungal species.
    • Low propensity for P450 drug-drug interactions.

    VL-2397 (ASP2397)

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