Synthetic intermediates of angustatin for antifungal research

Technology
Conceptual
University

Synthetic intermediates from the synthesis of Angustatin, a macrocyclic bisbibenzyl natural product with antifungal activity against Candida albicans. These simplified compounds are explored for their potential biological activity, offering opportunities for antifungal drug discovery and natural product chemistry collaborations.

Overview

This research focuses on the synthesis of Angustatin, a macrocyclic bisbibenzyl natural product originally isolated from the liverwort Asterella angusta. The project aims to prepare Angustatin through the shortest viable synthetic route using state-of-the-art metal catalysis. A key secondary objective is to evaluate the biological activity of the simpler intermediates generated during the synthesis, given that Angustatin itself exhibits antifungal properties against Candida albicans. These intermediates may retain or exhibit related antifungal activities, making them valuable candidates for further pharmacological investigation and potential lead compound development.

Technical specifications

Research approach:

  • Application of modern metal-catalyzed reactions to achieve an efficient total synthesis of Angustatin
  • Focus on minimizing synthetic steps while maximizing yield and selectivity
  • Generation and characterization of simplified intermediates along the synthetic pathway
  • Evaluation of intermediates for antifungal activity, particularly against Candida albicans
  • Exploration of the broader biological activity profile of Angustatin and its intermediates

Key features:

  • Access to novel macrocyclic bisbibenzyl scaffolds via streamlined synthesis
  • A library of structurally related intermediates available for biological screening
  • Potential for identifying new antifungal compounds with simplified structures
  • Integration of synthetic chemistry with natural product biology
Technology readiness level

The research is at an early-to-mid stage of development. Synthetic routes have been attempted and intermediates have been prepared, but further validation is needed to fully characterize the biological activity of both Angustatin and its intermediates. Future work includes completing the total synthesis, systematically screening intermediates for antifungal and other biological activities, and exploring structure-activity relationships to guide potential drug development efforts.


About Georg-August-Universität Göttingen

Georg‑August‑Universität Göttingen is a comprehensive public research university in Lower Saxony with broad academic breadth and a major university medical center. Through the Göttingen Campus alliance, the university is co‑located with Max Planck and Leibniz institutes, supported by a shared research data center that links campus partners and services. Clinical translation is enabled by the University Medical Center Göttingen, while proximity to leading life‑science and precision‑measurement companies in the region supports applied collaboration and talent pipelines. The university’s research is supported by competitive funding from the German Research Foundation, federal ministries, and European programmes. Technology transfer is provided by MBM ScienceBridge, a wholly owned subsidiary that manages IP, licensing, and startup support.

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