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Daher SS , Franklin KP , Scherzi T , Dunman PM , Andrade RB
Synthesis and biological evaluation of semi-synthetic albocycline analogs
Bioorg Med Chem Lett. 2020 Nov 1;30(21) :127509
PMID: 32827630 PMCID: PMC7577960 URL: https://www.ncbi.nlm.nih.gov/pubmed/32827630
AbstractAlbocycline (ALB) is a unique macrolactone natural product with potent, narrow-spectrum activity against methicillin-resistant Staphylococcus aureus (MRSA), vancomycin-intermediate (VISA), and vancomycin-resistant S. aureus (VRSA) strains (MIC = 0.5-1.0 μg/mL). Described herein is the synthesis and evaluation of a novel series analogs derived from albocycline by functionalization at three specific sites: the C2-C3 enone, the tertiary carbinol at C4, and the allylic C16 methyl group. Exploration of the structure-activity relationships (SAR) by means of minimum inhibitory concentration assays (MICs) revealed that C4 ester analog 6 was twice as potent as ALB, which represents a class of lead compound that can be further studied to address multi-drug resistant pathogens.
Notes1464-3405 Daher, Samer S Franklin, Kevin P Scherzi, Tyler Dunman, Paul M Andrade, Rodrigo B Journal Article England Bioorg Med Chem Lett. 2020 Aug 19:127509. doi: 10.1016/j.bmcl.2020.127509.