# First Enantioselective Syntheses of Bactobolins A, B, and Analogue Antibiotics

> **NIH NIH P20** · UNIVERSITY OF KANSAS LAWRENCE · 2020 · $154,892

## Abstract

Since the commercialization of penicillin in 1928, antibiotics have been hailed as “magic bullets”. In recent 
years, however, the number of bacterial strains resistant to clinically used antibiotics has sharply increased. 
The lack of viable first-line treatments of these bacterial infections has forced clinicians to consider secondline 
antibiotic options such as polymyxins and aminoglycosides, traditionally avoided because of significant 
toxicity. Thus, the development of antibiotics with new mechanisms of action for the control of pernicious 
bacterial infections is of vital importance. The synthesis of natural products and simplified derivatives has 
been a very successful strategy for the enrichment of the anti-infective armamentarium; a variety of clinically 
used antibacterial, antimalarial, and antifungal compounds have their origins in natural molecules. The 
specific aims of this proposal are: 1. Completion of the first enantioselective syntheses of Bactobolins A and 
B, two broad spectrum natural product antibiotics whose mechanism of action is the inhibition of protein 
translation via binding to an unprecedented site of the 50S ribosomal subunit and displacing tRNA bound at 
the P site. 2. Generation and evaluation of a plethora of functional analogues for future medicinal chemistry 
efforts. The rationale for this proposed research is that its success would allow for access to a diverse 
collection of antibacterial compounds with modes of action that are likely mechanistically distinct from FDAapproved 
antibiotics. The expected outcome of this research is the completion of several important steps 
towards the timely development of new, broad-spectrum, tolerable antibiotics. The successful execution of 
the research proposed herein is expected to have a significant positive impact by aiding the global effort to 
reduce human morbidity and mortality resulting from pernicious bacterial infections.

## Key facts

- **NIH application ID:** 10251389
- **Project number:** 5P20GM113117-05
- **Recipient organization:** UNIVERSITY OF KANSAS LAWRENCE
- **Principal Investigator:** Shyam Sathyamoorthi
- **Activity code:** P20 (R01, R21, SBIR, etc.)
- **Funding institute:** NIH
- **Fiscal year:** 2020
- **Award amount:** $154,892
- **Award type:** 5
- **Project period:** 2020-07-01 → 2021-07-31

## Primary source

NIH RePORTER: https://reporter.nih.gov/project-details/10251389

## Citation

> US National Institutes of Health, RePORTER application 10251389, First Enantioselective Syntheses of Bactobolins A, B, and Analogue Antibiotics (5P20GM113117-05). Retrieved via AI Analytics 2026-05-24 from https://api.ai-analytics.org/grant/nih/10251389. Licensed CC0.

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