Literature DB >> 32827630

Synthesis and biological evaluation of semi-synthetic albocycline analogs.

Samer S Daher1, Kevin P Franklin1, Tyler Scherzi2, Paul M Dunman2, Rodrigo B Andrade3.   

Abstract

Albocycline (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.
Copyright © 2020 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  Albocycline; Antibiotic; MIC; SAR

Mesh：

Substances：

Year:  2020        PMID： 32827630      PMCID： PMC7577960          DOI： 10.1016/j.bmcl.2020.127509

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


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