Journal
RSC ADVANCES
Volume 9, Issue 12, Pages 6770-6778Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c8ra10525a
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Funding
- Science & Technology Development Funds (STDF-Egypt)
- Egyptian Ministry of Higher Education and Scientific Research (MHESR)
- USAID
- NAS
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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 g 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 (C-max) that exceeds the MIC values.
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