Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 3, Issue 10, Pages 818-822Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ml3001775
Keywords
totarol; antimicrobial activity; small molecule inhibitors; FtsZ; structure-activity relationships and optimization
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Funding
- NIH/NIAID [R01AI08093]
- NIH/NIGMS [T32-GM008799]
- UC Davis
- United States Department of Education
- Alfred P. Sloan foundation
- NIH/NEI [EY012347]
- NIH [1DP2OD008735-01]
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The synthesis and antimicrobial activity of heterocyclic analogues of the diterpenoid totarol are described. An advanced synthetic intermediate with a ketone on the A-ring is used to attach fused heterocycles, and a carbon-to-nitrogen atom replacement is made on the B-ring by de nova synthesis. A-ring analogues with an indole attached exhibit, for the first time, enhanced antimicrobial activity relative to the parent natural product. Preliminary experiments demonstrate that the indole analogues do not target the bacterial cell division protein FtsZ as had been hypothesized for totarol.
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