Semisynthetic polymyxins with potent antibacterial activity and reduced kidney cell toxicity

Author:

Slingerland Cornelis J.1ORCID,Lysenko Vladyslav1,Chaudhuri Samhita1,Wesseling Charlotte M. J.1,Barnes Devon2,Masereeuw Rosalinde2ORCID,Martin Nathaniel I.1ORCID

Affiliation:

1. Biological Chemistry Group, Institute of Biology Leiden, Leiden University, Sylviusweg 72, 2333 BE Leiden, The Netherlands

2. Division of Pharmacology, Utrecht Institute of Pharmaceutical Sciences, Utrecht University, 3584 CG, Utrecht, The Netherlands

Abstract

A novel series of polymyxin analogues bearing a disulfide linked lipid tail are reported. The most promising variant identified exhibits antibacterial activity equipotent to that of polymyxin B and is >10-fold less toxic towards kidney cells.

Funder

H2020 European Research Council

Publisher

Royal Society of Chemistry (RSC)

Subject

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

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