Transition Metals and Antifungal Drug Design
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Questions and Answers

Who is the author of the study on the design of novel antifungal drugs?

Dr. Frans Hochstenbach

The insulin hexamer contains two zinc ions, each coordinated by three ______ residues.

His

Which of the following are current antifungals? (Select all that apply)

  • Nystatin (correct)
  • Amphotericin B (correct)
  • Miconazole (correct)
  • Penicillin
  • What is amphotericin B used for?

    <p>Therapy for systemic fungal infections</p> Signup and view all the answers

    Candicidin is currently in Phase I clinical trials.

    <p>False</p> Signup and view all the answers

    Which ions can leak through the pore formed by amphotericin B? (Select all that apply)

    <p>K+</p> Signup and view all the answers

    Match the following antifungal drugs with their type:

    <p>Nystatin = Polyene Fluconazole = Azole Miconazole = Azole Amphotericin B = Polyene Itraconazole = Azole</p> Signup and view all the answers

    Azoles are heterocycles of carbon and ______ atoms.

    <p>nitrogen</p> Signup and view all the answers

    What characteristic distinguishes miconazole from fluconazole?

    <p>Miconazole is a diazole, while fluconazole is a triazole.</p> Signup and view all the answers

    Study Notes

    Transition Metals

    • Transition metals are found in many biological processes
    • Insulin hexamer contains two zinc ions, each coordinated by three His residues
    • In manganese superoxide dismutase, the cofactor manganese is bound by three histidine side chains and one aspartate side chain.

    Antifungal Drug Design

    • Current antifungals include polyenes and azoles
    • Polyenes include nystatin, amphotericin B, candicidin, SPK-843

    Amphotericin B

    • Amphotericin B is a polyene used for systemic fungal infections
    • It forms a conducting pore in the plasma membrane of fungal cells
    • The pore is formed by two rings of eight amphotericin B molecules linked hydrophobically to ergosterol
    • The pore allows ions such as K+ and Mg2+ to leak out of the fungal cell, resulting in cell death

    Candicidin

    • Candicidin is a polyene in phase III clinical trials
    • Candicidin is more soluble than amphotericin B

    Azoles

    • Azoles are heterocycles of carbon and nitrogen atoms
    • Key examples include:
      • Miconazole (diazole)
      • Fluconazole (triazole)

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    Description

    Explore the role of transition metals in biological processes and their significance in antifungal drug design. This quiz discusses various antifungal agents, including polyenes and azoles, along with specific drugs like Amphotericin B and Candicidin. Test your knowledge on their mechanisms and chemical structures.

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