Antimycobacterial Activities of Novel 5-(1H-1,2,3-Triazolyl)Methyl Oxazolidinones

Table 3

In vivo bioavailability of selected oxazolidinones.

Compd.	~ MIC (𝜇g/mL) − serum	~ MIC (𝜇g/mL) + serum	Dilution factor^a	~ Compd in serum (𝜇g/mL)	Bioavailability^b
1g	1.1	3.3	1 : 20	22	low
1i	3.3	3.3	0	0	none
1o	0.37	3.3	0	0	none
2b	3.3	3.3	0	0	none
2j	1.1	1.1	0	0	none
2k	1.1	1.1	0	0	none
2l	1.1	0.37	1 : 10	11	low
3a	0.37	1.1	0	0	none
PH-27	1.1	0.37	1 : 80	88	medium
LZD	0.37	0.37	1 : 320	118.4	high
INH	0.014	0.041	1 : 320	4.48	high

^aDilution factor represents the last dilution step of the serum samples in which drug activity was still observed in the bioassay. (Drug levels in mouse serum are estimated by multiplying the dilution factor by the MIC value of the drug in absence of serum).
^bRating of bioavailability: low: activity of drug can be seen in 1 or 2 wells of the bioassay; medium: activity of drug can be seen in 3 or 4 wells of the bioassay; high: activity of drug can be seen in 5 or 6 wells.