Antimycobacterial activity of some pyrido-1,2-thiazine derivatives.
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.
Malinka
Wiesław
W
Department of Chemistry of Drugs, Wroclaw Medical University, 1 Tamka Str., 50-137 Wrocław, Poland.
Redzicka
Aleksandra
A
Swiatek
Piotr
P
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000494:pharmacology; D007202:Indicators and Reagents; D008826:Microbial Sensitivity Tests; D009161:Mycobacterium / Q000187:drug effects*; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D013843:Thiazines / Q000138:chemical synthesis* / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D000995:Antitubercular Agents; D007202:Indicators and Reagents; D011725:Pyridines; D013843:Thiazines; C473150:pyrido-1,2-thiazine