title: Flavimycins A and B, dimeric 1,3-dihydroisobenzofurans with peptide deformylase inhibitory activity from Aspergillus flavipes.
abstract: Flavimycins A (1) and B (2), novel dimeric 1,3-dihydroisobenzofurans, were isolated as inhibitors of peptide deformylase from cultures of Aspergillus flavipes. Their chemical structures were established by NMR and MS data analysis. Compounds 1 and 2 exist as epimeric mixtures at C-1 through fast hemiacetal-aldehyde tautomerism. Compounds 1 and 2 inhibited Staphylococcus aureus peptide deformylase with IC₅₀ values of 35.8 and 100.1 μM, respectively. Consistent with their PDF inhibition, 1 showed two times stronger antibacterial activity than 2 on S. aureus including MRSA, with MIC values of 32-64 μg/mL.
authors.affiliation: Korea Research Institute of Bioscience and Biotechnology , Yusong, Daejeon 305-806, Republic of Korea.
authors.forename: Yun-Ju
authors.initials: YJ
authors.lastname: Kwon
authors.forename: Mi-Jin
authors.initials: MJ
authors.lastname: Sohn
authors.forename: Chang-Jin
authors.initials: CJ
authors.lastname: Kim
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Koshino
authors.forename: Won-Gon
authors.initials: WG
authors.lastname: Kim
mesh_terms: D000581:Amidohydrolases / Q000037:antagonists & inhibitors; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology*; D001230:Aspergillus / Q000737:chemistry*; D001572:Benzofurans / Q000737:chemistry / Q000302:isolation & purification / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D056910:Republic of Korea; D013211:Staphylococcus aureus / Q000187:drug effects*; D013237:Stereoisomerism
chemical_list: D000900:Anti-Bacterial Agents; D001572:Benzofurans; C571475:flavimycin A; C571476:flavimycin B; D000581:Amidohydrolases; C084507:peptide deformylase