# SYNTHETIC STUDIES ON THE POLYENE MACROLIDE ANTIBIOTICS

> **NIH NIH R01** · UNIVERSITY OF VIRGINIA · 1989 · $118,845

## Abstract

The goal is to gain an understanding at the molecular level of the
mechanism of action of the antifungal properties associated with the
polyene macrolide antibiotics.  The design and synthesis of unnatural
compounds will be pursued with the objective of realizing antifungal agents
of improved therapeutic efficacy.  This study is simultaneously pursuing
three interrelated avenues of investigation:  a.  the development of a
general synthetic approach the polyene macrolide class of antibiotics, b.
the synthesis of simplified polyene macrolide analogs, and c.  physical
studies aimed at understanding the structural details of the critical
polyene-sterol interactions required for fungicidal activity.  Within the
context of the synthetic studies, general problems in acyclic asymmetric
synthesis are being addressed, principally through diastereoselective
elaboration of L-aspartic acid.  As synthetic methodology is developed,
access to increasingly diverse analogs to the natural polyene macrolides
becomes available to test the structural features of these compounds that
lead to selective binding with certain sterols.  These studies are further
supported by spectroscopic (i.e., NMR) efforts to directly observe the
polyene-sterol pairs in solution, micelles, and in membranes.

## Key facts

- **NIH application ID:** 3127297
- **Project number:** 5R01AI017595-09
- **Recipient organization:** UNIVERSITY OF VIRGINIA
- **SAM.gov UEI:** JJG6HU8PA4S5
- **Principal Investigator:** GLENN J MC GARVEY
- **Activity code:** R01 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 1989
- **Award amount:** $118,845
- **Award type:** 5
- **Project period:** 1980-12-01 → 1991-11-30

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/3127297

## Citation

> US National Institutes of Health, RePORTER application 3127297, SYNTHETIC STUDIES ON THE POLYENE MACROLIDE ANTIBIOTICS (5R01AI017595-09). Retrieved via MORVS 2026-10-25 from https://api.morvs.ai/grant/nih/3127297. Licensed CC0.

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