Abstract
2-Ethylsulfonyl-7-methyl-5H-1, 3, 4-thiadiazolo[3, 2-a]pyrimidin-5-one (TPSO2 − 2) showed inhibitory activity on cellular respiration of Ehrlich ascites tumor cells (E-cells) and Escherichia coli at 3.9 × 10−4 m. In polarographic traces of rat liver mitochondrial respiration, the agent inhibited the energy transfer of oxidative phosphorylation at 8 × 10−4 m. However, in the presence of tricine[N-tris(hydroxymethyl)methylglycine], the TPSO2 − 2 inhibitory activity on cellular respiration disappeared. The permeability of cells was altered by TPSO2 − 2 treatment, and this effect was interrupted by adding tricine. TPSO2 − 2 did not inhibit the multiplication of E. coli in the presence of tricine but did inhibit E-cell multiplication. This means that the inhibitory activity of TPSO2 − 2 on E. coli multiplication is attributable to respiration inhibition, whereas the cytotoxicity of TPSO2 − 2 should be due to reasons other than respiration inhibition.
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