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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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Contributor : Marie-Lise Bourguet-Kondracki Connect in order to contact the contributor
Submitted on : Tuesday, November 24, 2020 - 9:52:49 AM
Last modification on : Thursday, July 7, 2022 - 6:02:26 AM
Long-term archiving on: : Thursday, February 25, 2021 - 6:51:39 PM


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Melissa M Cadelis, Elliot I W 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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