Synthesis of novel isothiazolopyridines and their in vitro evaluation against Mycobacterium and Propionibacterium acnes |
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Authors: | Wies?aw Malinka Piotr ?wi?tek Ma?gorzata ?liwińska Bogumi?a Szponar Andrzej Gamian Zbigniew Karczmarzyk Andrzej Fruziński |
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Institution: | 1. Department of Chemistry of Drugs, Wroc?aw Medical University, Borowska 211, 50-556 Wroc?aw, Poland;2. Institute of Immunology and Experimental Therapy, Polish Academy of Sciences, Weigla 12, 53-114 Wroc?aw, Poland;3. Department of Medical Biochemistry, Wroc?aw Medical University, Cha?ubińskiego 10, 50-368 Wroc?aw, Poland;4. Department of Chemistry, University of Podlasie, 3 Maja 54, 08-110 Siedlce, Poland;5. Institute of General and Ecological Chemistry, Technical University, ?eromskiego115, 90-924 ?ód?, Poland;6. College of Physiotherapy, Ko?ciuszki 4, 50-038 Wroc?aw, Poland |
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Abstract: | In this paper we describe synthesis, structures and some physicochemical properties of 20 isothiazolopyridines 8–13 substituted differently into an isothiazole ring as well as their in vitro antibacterial assays against Mycobacterium tuberculosis H37Rv, Mycobacterium fortuitum PCM 672 and Propionibacterium acnes PCM 2400. Compound 13a was found to be the most active derivative against M. tuberculosis H37Rv, demonstrating 100% growth inhibition of microorganisms in the primary screen (minimum inhibitory concentration MIC] 6.25 μg/mL). Nineteen of the prepared compounds were evaluated against M. fortuitum PCM 672 and P. acnes PCM 2400 and only compounds 9 and 12d exhibited excellent activity against individual strains of microorganisms with MIC90 <1 μg/mL. The inhibitory action of the remaining isothiazolopyridines towards the tested strains of the microorganism was low, absent, or a non-linear correlation prohibited accurate determination of MIC values. Unexpectedly, seven of the remaining isothiazolopyridines tested against M. fortuitum and P. acnes stimulated growth of the microorganisms in the range 10–50% or even more (10b) under experimental conditions. |
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Keywords: | Isothiazolopyridine Synthesis Antibacterial activity Antimycobacterial agents |
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