Direct modifications of the cyclic peptide Polymyxin B leading to analogues with enhanced in vitro antibacterial activity.

Bioorg Med Chem Lett

Cantab Anti-Infectives Ltd, Welwyn Garden City AL7 3AX, UK; Spero Therapeutics, Inc, 675 Massachusetts Avenue, 14th Floor, Cambridge, MA 02139 USA.

Published: June 2020

AI Article Synopsis

  • Synthetic modifications to the cyclic peptide core of polymyxin B have deepened the understanding of its structure-activity relationships.
  • These modified versions of polymyxin B can be broken down by enzymes, allowing for the creation of various semi-synthetic analogues.
  • The resulting compounds from these modifications show improved antibacterial activity in lab tests.

Article Abstract

Synthetic modifications have been made directly to the cyclic peptide core of polymyxin B, enabling the further understanding of structure activity relationships of this antimicrobial peptide. Such modified polymyxins are also substrates for enzymic hydrolysis, enabling the synthesis of a variety of semi-synthetic analogues, resulting in compounds with increased in vitro antibacterial activity.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7215238PMC
http://dx.doi.org/10.1016/j.bmcl.2020.127163DOI Listing

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