Semisynthetic blasticidin S ester derivatives show enhanced antibiotic activity

Author:

Gannett Cole12ORCID,Banks Paige1,Chuong Christina32,Weger-Lucarelli James32,Mevers Emily124,Lowell Andrew N.124ORCID

Affiliation:

1. Department of Chemistry, Virginia Polytechnic Institute and State University (Virginia Tech), Blacksburg, VA 24061, USA

2. Center for Emerging, Zoonotic, and Arthropod-borne Pathogens, Virginia Polytechnic Institute and State University (Virginia Tech), Blacksburg, VA 24061, USA

3. Department of Biomedical Sciences and Pathobiology, VA-MD Regional College of Veterinary Medicine, Virginia Polytechnic Institute and State University (Virginia Tech), Blacksburg, VA 24061, USA

4. Faculty of Health Sciences, Virginia Polytechnic Institute and State University (Virginia Tech), Blacksburg, VA 24061, USA

Abstract

A potential rich source of new antimicrobials is undeveloped natural product cytotoxins. We used semisynthesis to derivatize the neglected antibiotic blasticidin S, creating ester derivatives with enhanced selectivity for bacteria.

Funder

Virginia Polytechnic Institute and State University

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry,Drug Discovery,Pharmaceutical Science,Pharmacology,Molecular Medicine,Biochemistry

Reference18 articles.

1. The global preclinical antibacterial pipeline

2. Global burden of bacterial antimicrobial resistance in 2019: a systematic analysis

3. 2020 Antibacterial Agents in Clinical and Preclinical Development: An Overview and Analysis , World Health Organization , Geneva , 2021 , licence: CC BY-NC-SA 3.0 IGO

4. Natural Products as Sources of New Drugs over the Nearly Four Decades from 01/1981 to 09/2019

5. Antibiotics: past, present and future

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