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Exploration of the antibiotic potentiating activity of indolglyoxylpolyamines

Abstract : A series of substituted di-indolglyoxylamido-spermine analogues were prepared and evaluated for intrinsic antimicrobial properties and the ability to enhance antibiotic action. As a compound class, intrinsic activity was typically observed towards Gram-positive bacteria and the fungus Cryptococcus neoformans, with notable exceptions being the 5-bromo-and 6-chloro-indole analogues which also exhibited modest activity (MIC 34-50 µM) towards the Gram-negative bacteria Escherichia coli and Klebsiella pneumoniae. Several analogues enhanced the activity of doxycycline towards the Gram-negative bacteria Pseudomonas aeruginosa, E. coli, K. pneumoniae and Acinetobacter baumannii. Of particular note was the identification of five antibiotic enhancing analogues (5-Br, 7-F, 5-Me, 7-Me, 7-OMe) which also exhibited low to no cytotoxicity and red blood cell haemolytic properties. The mechanisms of action of the 5-Br and 7-F analogues were attributed to the ability to disrupt the integrity of, and depolarize, bacterial membranes.
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https://hal-cnrs.archives-ouvertes.fr/hal-03020885
Contributor : Marie-Lise Bourguet-Kondracki <>
Submitted on : Tuesday, November 24, 2020 - 9:52:49 AM
Last modification on : Thursday, December 3, 2020 - 4:02:04 PM

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Melissa Cadelis, Elliot Pike, Weirong Kang, Zimei Wu, Marie-Lise Bourguet-Kondracki, et al.. Exploration of the antibiotic potentiating activity of indolglyoxylpolyamines. European Journal of Medicinal Chemistry, Elsevier, 2019, 183, pp.111708. ⟨10.1016/j.ejmech.2019.111708⟩. ⟨hal-03020885⟩

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