Modular Synthesis and First Antimicrobial Investigation of Mycoleptodiscin A and Simplified Indolosesquiterpenoids

06 March 2024, Version 1
This content is a preprint and has not undergone peer review at the time of posting.


The structure-activity relationship of the structurally unusual indolosesquiterpenoid mycoleptodiscin A is unknown due to natural scarcity and inefficient synthesis. A modular approach leveraging Larock indole synthesis has been established to access mycoleptodiscin A and a divergent collection of unprecedented drimanyl indoles. This tactic features the utilization of a commercially available and inexpensive (+)-sclareolide, modularity, purification-economy, and scalability, which facilitates the first biological evaluation of mycoleptodiscin A and related pseudo-natural products for identification of promising new leads.


mycoleptodiscin A
modular synthesis
antimicrobial investigation


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