Journal
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
Volume 130, Issue 39, Pages 13110-13119Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ja8044376
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Funding
- National Institutes of Health (USA)
- National Science Foundation [CHE-0603217]
- Skaggs Institute for Chemical Biology
- Bristol-Myers Squibb
- Schering AG
- Spanish Ministry of Science and Education
- Merck Sharp Dohme
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The molecular design, chemical synthesis, and biological evaluation of two distinct series of platensimycin analogues with varying degrees of complexity are described. The first series of compounds probes the biological importance of the benzoic acid subunit of the molecule, while the second series explores the tetracyclic cage domain. The biological data obtained reveal that, while the substituted benzoic acid domain of platensimycin is a highly conserved structural motif within the active compounds with strict functional group requirements, the cage domain of the molecule can tolerate considerable structural modifications without losing biological action. These findings refine our present understanding of the platensimycin pharmacophore and establish certain structure-activity relationships from which the next generation of designed analogues of this new antibiotic may emerge.
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