Synthesis and antibacterial evaluation of a novel series of 2-(1,2-dihydro-3-oxo-3H-pyrazol-2-yl)benzothiazoles |
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Authors: | Stella Alessandro Segers Kenneth De Jonghe Steven Vanderhoydonck Bart Rozenski Jef Anné Jozef Herdewijn Piet |
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Affiliation: | Katholieke Universiteit Leuven, Rega Institute for Medical Research, Laboratory of Medicinal Chemistry, Minderbroedersstraat 10, Leuven, Belgium. |
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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 μM . |
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Keywords: | Benzothiazoles, 2‐(3‐oxopyrazol‐2‐yl)‐ Antibacterial activity Structure–activity relationship (SAR) |
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