Antifungal, Antiparasitic, antimycobacterium Medicinal Chemistry

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Antifungal, Antiparasitic, antimycobacterium Medicinal Chemistry
2011-04-13 10:45:42
antifungal antiparasitic antimycobacterium medicinal chemistry

Antifungal, Antiparasitic, Antimycobacterium Medicinal Chemistry
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  1. Amphotericin B
    • Polyene antifungal
    • Disrupt ergosterol
    • Highly toxic; cannot cross the BBB
  2. Ketoconazole
    CYP 14-alpha-demethylase inhibitor
  3. Fluconazole
    • CYP 14-alpha-demethylase inhibitor
    • Can cross BBB
    • Resistance: mutations in how heme/drug fits in the binding site
  4. Terbinafine
    • Squalene epoxidase inhibitors
    • Inhibit both ergosterol and cholesterol biosynthesis.
  5. Voriconazole
    CYP 14-alpha-demethylase inhibitorCan cross BBB
  6. Echinacins
    Inhibit beta-1,3-Glycan synthase cell wall biosynthesis
  7. Flucytosine
    Converted into 5-fluorouracil (antimetabolite)
  8. Isoniazid
    Inhibit inhA by imitating NADH
  9. Rifampin
    • Inhibit DNA-dependent RNA polymerase
    • Cap that fits over a part of protein in DDRP that's important for reading DNA
    • Resistance: mutation
  10. Ethambutol
    • Inhibition of mycobacterial cell wall biosynthesis (arabinosyltransferease)
    • Resistance: overexpression of arabinosyl transferase
  11. Ethionamide
    Inhibition of inhA
  12. Cycloserine
    • Competitive inhibition of D-alanine racemase and D-alanine ligase
    • CNS side effects
  13. Nitroimidazoles
    Fragmentation of DNA
  14. Atovaquone
    Inhibits protozoa ubiquinone reductase in the mitochondrial respiratory chain
  15. Pentamidine
    Inhibition of topoisomerase
  16. Trimetrexate
    Inhibit DHF
  17. Eflornithine
    • Inhibitor of ornithine decarboxylase
    • Cofactor: pyridoxyl-5-phosphate
  18. Nifurtimox
    ROS mechanism to fragment DNA
  19. Benznidazole
    Does not work through a ROS mechanism
  20. Melarsoprol
    Inhibition of a pyruvate kinase in trypanosomal glycolysis
  21. Sodium stibogluconate and meglumine antimonate
    Inhibition of bioenergetic processes, including glycolytic enzymes
  22. Ivermectin
    Reduces motility of microfalaria through action at nematode GABA receptors.
  23. Praziquantel
    Ca redistribution, leading to worm muscle contraction and paralysis, leading to worm expulsion.
  24. Lindane
    Insecticide that stimulates insect CNS GABA receptors