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Issue 12, 2019
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tert-Butylphenylthiazoles with an oxadiazole linker: a novel orally bioavailable class of antibiotics exhibiting antibiofilm activity

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Abstract

The structure–activity and structure–kinetic relationships of a new tert-butylphenylthiazole series with oxadiazole linkers were conducted with the objective of obtaining a new orally available antibacterial compounds. Twenty-two new compounds were prepared, purified and identified. Their activity against methicillin-resistant Staphylococcus aureus were examined. Compound 20 with 3-hydroxyazetidine as a nitrogenous side chain showed promising activity against twenty-four clinical isolates, including vancomycin-resistant staphylococcal and enterococcal species with MIC values ranging from 4–8 μg mL−1. Additional advantages of this compound include an ability to eradicate staphylococcal biofilm mass in a dose-dependent manner as well as high metabolic stability after an oral dose of 25 mg kg−1 with a biological half-life that exceeds 5 hours and a plasma concentration (Cmax) that exceeds the MIC values.

Graphical abstract: tert-Butylphenylthiazoles with an oxadiazole linker: a novel orally bioavailable class of antibiotics exhibiting antibiofilm activity

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Supplementary files

Article information


Submitted
23 Dec 2018
Accepted
16 Feb 2019
First published
26 Feb 2019

This article is Open Access

RSC Adv., 2019,9, 6770-6778
Article type
Paper

tert-Butylphenylthiazoles with an oxadiazole linker: a novel orally bioavailable class of antibiotics exhibiting antibiofilm activity

A. Kotb, N. S. Abutaleb, M. Hagras, A. Bayoumi, M. M. Moustafa, A. Ghiaty, Mohamed N. Seleem and A. S. Mayhoub, RSC Adv., 2019, 9, 6770
DOI: 10.1039/C8RA10525A

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