# Total Synthesis of Bioactive Indole Alkaloids and Application as Agrochemicals

> **NIH NIH F31** · UNIVERSITY OF CALIFORNIA BERKELEY · 2023 · $13,033

## Abstract

PROJECT SUMMARY/ABSTRACT
Agrochemicals are used in industrial food production to ensure the world has access to ample, healthy food.
One major problem that drives development of novel agrochemicals is pesticide resistance. As a result, novel
mechanisms of action (MoA) are highly sought-after in order to circumvent resistance to existing agrochemicals.
To this end, natural products often serve as sources for identifying compounds active toward these novel MoAs.
Calcium channels have been identified as under-exploited targets for insecticides and serve as viable, novel
MoAs. Scholarinine A, an akuammiline monoterpenoid indole alkaloid, has been identified as a platform for the
development of insecticides with novel MoAs due to its’ ability to inhibit calcium channels. A synthesis campaign
towards this natural product and structurally related indole alkaloids will enable initial screening toward an insect
calcium channel inhibitor. These studies will be accomplished through three specific aims: 1) completing the total
synthesis of scholarinine A, 2) synthesizing structurally related natural products and performing initial biological
assays, and 3) derivatizing the indole alkaloids to conduct structure activity relationship studies through
collaborative efforts with Corteva AgriSciences.
The total synthesis of scholarinine A and other akuammiline indole alkaloids will be pursued through the
execution of a key cyclization cascade to forge the carbocyclic framework of the natural products, followed by
late-stage peripheral functionalizations. Development of a divergent route to structurally related indole alkaloids
will allow for biological evaluation of these compounds for application as insecticides. Additionally, development
of a synthetic route will lay the foundation for biological testing of these compounds as therapeutics for
neurological disorders associated with calcium channel dysregulation in the future. In the end, synthesis and
biological testing of these indole alkaloids will provide crucial information on the calcium channel inhibitory
capabilities of these compounds.

## Key facts

- **NIH application ID:** 10620698
- **Project number:** 5F31GM146406-02
- **Recipient organization:** UNIVERSITY OF CALIFORNIA BERKELEY
- **Principal Investigator:** Kerry E. Jones
- **Activity code:** F31 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2023
- **Award amount:** $13,033
- **Award type:** 5
- **Project period:** 2022-05-01 → 2023-05-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10620698

## Citation

> US National Institutes of Health, RePORTER application 10620698, Total Synthesis of Bioactive Indole Alkaloids and Application as Agrochemicals (5F31GM146406-02). Retrieved via AI Analytics 2026-05-22 from https://api.ai-analytics.org/grant/nih/10620698. Licensed CC0.

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