Isolation and Identification of FR198248, a Hydroxylated 1,3-Dihydroisobenzofuran, from Aspergillus flavipes as an Inhibitor of Peptide Deformylase

Abstract

Two highly hydroxylated 1,3-dihydroisobenzofurans, FR198248 (1) and FR202306 (2), were isolated as peptide deformylase (PDF) inhibitors from Aspergillus flavipes. Compounds 1 and 2 inhibited Staphylococus aureus PDF with IC₅₀ values of 3.6 and 2.5 μM, respectively, and also showed antibacterial activity with an MIC value of 25 μg/ml. In contrast, 6-O-methyl derivative 3 of compound 2 was inactive against both PDF and S. aureus.