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Antimycobacterial activity of some pyrido-1,2-thiazine derivatives
Wiesław Malinka1, Aleksandra Redzicka, Piotr Swiatek
1Department of Chemistry of Drugs, Wroclaw Medical University, 1 Tamka Str., 50-137 Wrocław, Poland.
Abstract:
The 3-benzoylpyrido-1,2-thiazine-1,1-dioxides 1 and the related pyrazolopyrido-1,2-thiazine-5,5-dioxides 2 with a 4-arylpiperazin-1-ylpropyl side chained by the nitrogen atom of the thiazine ring were evaluated in vitro against Myobacterium tuberculosis H37Rv. Some of the tested compounds proved to be potent antimycobacterial agents and for the most active of them (1a,b) minimum inhibitory concentrations (MIC = 3.13 and 6.25 microg/ml, respectively) were determined. The correlation between mycobacterium growth inhibition and the lipophilicity (logPcalc.) within the series of derivatives 1 and 2 was studied.
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