Title: Synthesis and Antibacterial Evaluation of a Novel Series of 2-(1,2-Dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazoles
Authors: Stella, Alessandro
Segers, Kenneth
De Jonghe, Steven
Vanderhoydonck, Bart
Rozenski, Jef
Anné, Jozef
Herdewijn, Piet # ×
Issue Date: Mar-2011
Publisher: Verlag Helvetica Chimica Acta
Series Title: Chemistry & Biodiversity vol:8 issue:2 pages:253-265
Abstract: The 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazole scaffold was selected as a central core structure for the discovery of novel antibacterial compounds. A systematic variation of the substituents on the oxo-pyrazole moiety, as well as on the benzo moiety, led to the creation of a small and focused library of benzothiazoles that was subjected to antibacterial screening. In a first round of screening, activity of the compounds against six representative microorganisms was established. For the most potent congeners, MIC values against S. aureus and P. aeruginosa were determined. The structure-activity relationship study clearly revealed that subtle structural variations influence the antibacterial activity to a large extent. The most potent congeners displayed MIC values of 3.30 mu m.
ISSN: 1612-1872
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
Department of Pharmaceutical & Pharmacological Sciences - miscellaneous
Laboratory of Molecular Bacteriology (Rega Institute)
Interface Valorization Platform (IVAP) (-)
× corresponding author
# (joint) last author

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