PF-1163A | AnyMole

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HIT ID:HIT218832933
Cas No:
常用名:PF-1163A
IUPAC:3-{[4-(2-hydroxyethoxy)phenyl]methyl}-13-(2-hydroxypentyl)-4,10-dimethyl-1-oxa-4-azacyclotridecane-2,5-dione
IUPAC:3-{[4-(2-hydroxyethoxy)phenyl]methyl}-13-(2-hydroxypentyl)-4,10-dimethyl-1-oxa-4-azacyclotridecane-2,5-dione
InChI key:SDBGPLZSWIQIOV-UHFFFAOYSA-N

分子式:C27H43NO6
分子量:477.642
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:CCCC(O)CC1CCC(C)CCCCC(=O)N(C)C(Cc2ccc(OCCO)cc2)C(=O)O1
SMILES:CCCC(O)CC1CCC(C)CCCCC(=O)N(C)C(Cc2ccc(OCCO)cc2)C(=O)O1

PF-1163A, a depsipeptide antifungal compound isolated from Penicillium, blocks ergosterol synthesis with an IC50 of 12 ng/ml. This compound specifically inhibits the enzyme ERG25p, a C-4 methyl oxidase in the ergosterol biosynthetic pathway, leading to its antifungal activity. Notably, in Saccharomyces cerevisiae modified to express ERG biosynthesis genes, PF-1163A exhibits an inhibition concentration (MIC value) of 12.5 µg/ml against ERG25p, though strains overexpressing ERG25p show resistance. Additionally, PF-1163A effectively suppresses the growth of Candida albicans (MIC = 8 µg/ml), without affecting other Candida species, Aspergillus fumigatus, or HepG2 cells. Remarkably, it enhances the efficacy of fluconazole against azole-resistant C. albicans strains, showing a significant decrease in MICs (1 and 0.0078 µg/ml alone and in combination, respectively). PF-1163A distinguishes itself from PF-1163B by its more polar nature.

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