Isolation and identification of FR198248, a hydroxylated 1,3-dihydroisobenzofuran, from Aspergillus flavipes as an inhibitor of peptide deformylase.
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 IC(50) values of 3.6 and 2.5 microM, respectively, and also showed antibacterial activity with an MIC value of 25 microg/ml. In contrast, 6-O-methyl derivative 3 of compound 2 was inactive against both PDF and S. aureus.
Korea Research Institute of Bioscience and Biotechnology, Yusong, Daejon, Republic of Korea.
Yun-Ju
YJ
Kwon
Chang-Ji
CJ
Zheng
Won-Gon
WG
Kim
D000581:Amidohydrolases / Q000037:antagonists & inhibitors*; D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001230:Aspergillus / Q000737:chemistry*; D001572:Benzofurans / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects
D000900:Anti-Bacterial Agents; D001572:Benzofurans; C424923:FR 198248; D000581:Amidohydrolases; C084507:peptide deformylase