Antifungal, Antiparasitic, antimycobacterium Medicinal Chemistry
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- Polyene antifungal
- Disrupt ergosterol
- Highly toxic; cannot cross the BBB
CYP 14-alpha-demethylase inhibitor
- CYP 14-alpha-demethylase inhibitor
- Can cross BBB
- Resistance: mutations in how heme/drug fits in the binding site
- Squalene epoxidase inhibitors
- Inhibit both ergosterol and cholesterol biosynthesis.
CYP 14-alpha-demethylase inhibitorCan cross BBB
Inhibit beta-1,3-Glycan synthase cell wall biosynthesis
Converted into 5-fluorouracil (antimetabolite)
Inhibit inhA by imitating NADH
- Inhibit DNA-dependent RNA polymerase
- Cap that fits over a part of protein in DDRP that's important for reading DNA
- Resistance: mutation
- Inhibition of mycobacterial cell wall biosynthesis (arabinosyltransferease)
- Resistance: overexpression of arabinosyl transferase
Inhibition of inhA
- Competitive inhibition of D-alanine racemase and D-alanine ligase
- CNS side effects
Fragmentation of DNA
Inhibits protozoa ubiquinone reductase in the mitochondrial respiratory chain
Inhibition of topoisomerase
- Inhibitor of ornithine decarboxylase
- Cofactor: pyridoxyl-5-phosphate
ROS mechanism to fragment DNA
Does not work through a ROS mechanism
Inhibition of a pyruvate kinase in trypanosomal glycolysis
Sodium stibogluconate and meglumine antimonate
Inhibition of bioenergetic processes, including glycolytic enzymes
Reduces motility of microfalaria through action at nematode GABA receptors.
Ca redistribution, leading to worm muscle contraction and paralysis, leading to worm expulsion.
Insecticide that stimulates insect CNS GABA receptors
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