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EU funding (€286,191): Unlocking the Antitubercular Mode of Action of Asperterpenoid through Total Synthesis Hor 16 Apr 2024 EU Research and Innovation programme "Horizon"
Overview
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Unlocking the Antitubercular Mode of Action of Asperterpenoid through Total Synthesis
The rise of multi-drug resistant strains of Mycobacterium tuberculosis, the pathogen responsible for the infectious disease tuberculosis, calls for research into novel antitubercular scaffolds and targets. Asperterpenoid is a rare sesterterpenoid with a unique and highly complex 5/7(3)/6/5 ring-fused carbon skeleton that strongly inhibits tyrosine phosphatase B, a virulence factor protein secreted by M. tuberculosis that aids human host infection. To date, total synthesis of asperterpenoid has not been accomplished. We propose a modular synthesis of asperterpenoid from biorenewable sitolactone using a key intermolecular reductive titanium mediated Giese addition reaction. The scope of this privileged reaction will be expanded by investigating selected epoxide substrates and Michael acceptors. We anticipate that the synthetic strategy to asperterpenoid can be extrapolated to prepare variecolin, a structurally related sesterterpenoid that has been subject of several studies but never reached by chemical synthesis. Based on its structural similarity to asperterpenoid, we expect that variecolin will also exhibit antitubercular activity. We plan to study the known antitubercular activity of asperterpenoid by structural diversification and its mechanism of action by a chemical biology tools such as molecular imaging. We also plan to test variecolin for antitubercular activity. The action is expected to contribute to new synthetic tools and strategies to prepare rare sesterterpenoid natural products, a better understanding of the promising antitubercular properties of asperterpenoid, and to demonstrate that variecolin exhibits similar bioactive behaviour.
Funded Companies:
| Company name | Funding amount |
| THE Regents OF THE University OF California | ? |
| Aarhus Universitet | €286,191 |
Source: https://cordis.europa.eu/project/id/101150348
The filing refers to a past date, and does not necessarily reflect the current state. The latest known state is available on the following page: University OF California, Berkeley Foundation, Berkeley, United States.
