Polyheterocyclic peptidomimetics: Parallel solid phase synthesis of oligo cyclic guanidines and their inhibition activity against Mycobacterium tuberculosis DNA gyrase

Bioorg Med Chem Lett. 2023 Sep 1:93:129439. doi: 10.1016/j.bmcl.2023.129439. Epub 2023 Aug 8.

Abstract

Polyheterocycles are one of the most desired synthetic targets due to their numerous and valuable applications in various fields. We report the design and the parallel synthesis of novel linear oligocyclic guanidine peptidomimetics from predesigned reduced polyamides. A screening of these compounds identified active Mycobacterium tuberculosis DNA gyrase inhibitors which do not inhibit human DNA topoisomerase IIα and topoisomerase I.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • DNA Gyrase
  • Guanidine
  • Guanidines
  • Humans
  • Mycobacterium tuberculosis*
  • Peptidomimetics* / pharmacology
  • Peptidomimetics* / therapeutic use
  • Solid-Phase Synthesis Techniques
  • Topoisomerase II Inhibitors / pharmacology
  • Topoisomerase II Inhibitors / therapeutic use
  • Tuberculosis* / drug therapy

Substances

  • DNA Gyrase
  • Peptidomimetics
  • Guanidines
  • Topoisomerase II Inhibitors
  • Guanidine