Strong Antibiotic Activity of the Myxocoumarin Scaffold in vitro and in vivo

Autor:	Gesa Hertrampf, Kalina Kusserow, Sandra Vojnovic, Aleksandar Pavic, Jonas I. Müller, Jasmina Nikodinovic‐Runic, Tobias A. M. Gulder
Rok vydání:	2022
Předmět:	Methicillin-Resistant Staphylococcus aureus Biological Products Structure-Activity Relationship Organic Chemistry Animals General Chemistry Microbial Sensitivity Tests Catalysis Zebrafish Anti-Bacterial Agents
Zdroj:	Chemistry (Weinheim an der Bergstrasse, Germany). 28(32)
ISSN:	1521-3765
Popis:	The increasing emergence of resistances against established antibiotics is a substantial threat to human health. The discovery of new compounds with potent antibiotic activity is thus of utmost importance. Within this work, we identify strong antibiotic activity of the natural product myxocoumarin B from Stigmatella aurantiaca MYX-030 against a range of clinically relevant bacterial pathogens, including clinical isolates of MRSA. A focused library of structural analogs was synthesized to explore initial structure-activity relationships and to identify equipotent myxocoumarin derivatives devoid of the natural nitro substituent to significantly streamline synthetic access. The cytotoxicity of the myxocoumarins as well as their potential to cure bacterial infections in vivo was established using a zebrafish model system. Our results reveal the exceptional antibiotic activity of the myxocoumarin scaffold and hence its potential for the development of novel antibiotics.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d4ac5ec48466b0544fe4ef09c9e7108 https://pubmed.ncbi.nlm.nih.gov/35229915 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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