Chitin synthetase inhibitors : Nikomycin - Synthesis and Drug Profile
1. Nikomycin
Mode of action: Nikomycin competitively inhibits the chitin
synthase, mimicking its substrate uridine diphosphate-N-acetyl glucosamine of fungi with C. albicans as the primary target organism. The enzyme is an
integral membrane protein. Nikomycin Z has shown to act synergistically in
vitro with fluconazole, ketoconzole, and tioconazole against C. albicans at minimum inhibitory
concentration (MIC) levels of azoles.
Properties and uses: Nikomycin is a nucleoside peptide antibiotic
that is produced by soil strains of Steptomyces
tendae. It is found to be more potent than most azoles in inhibiting highly
chitinous, dimorphic fungal pathogens, such as Coccidiodes imitis and Blastomyces
dermatidis.
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