Tuberculosis Research and Treatment

Research Article

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

Table 2

In vitro antimycobacterium activity of 4N-arylcarbonyl- and 4N-arylsulfonyl-piperazinyl oxazolidinones against M. tuberculosis H37Rv.




Compd.	–R	values	IC₉₀ (g/mL)	CC₅₀ (g/mL) VERO	SI

2a	PhCO	0.6148	0.722	>45.04	>62.3
b	4-ClPhCO	1.4304	<0.20	>48.49	>242.4
c	3-NO₂PhCO	0.5198	0.759	>49.54	>65.27
d	2-CH₃PhCO	1.1138	3.375	>46.45	>13.76
e	3-CH₃PhCO	1.1138	0.422	>46.45	>110
f	4-CH₃PhCO	1.1138	2.103	>46.45	>22.08
g	2-CH₃OPhCO	0.8347	1.04	>48.05	>46.15
h	3-CH₃OPhCO	0.8347	0.829	>48.05	>57.89
i	4-CH₃OPhCO	0.8347	0.843	>48.05	>56.93
j	2-furylCO	−0.2092	<0.20	>44.04	>220.2
k	2-thienylCO	0.3913	0.209	>45.65	>217.3
l	3-pyridylCO	−0.4862	0.236	>45.14	>190.4
m	2-Cl 3-pyridylCO	0.2641	1.389	>48.59	>34.98
3a	CH₃SO₂	−0.6042	<0.20	>42.44	>212.2
b	2-furylSO₂	1.0658	>100 (0.419)^a	n/d	n/d
c	PhSO₂	1.3448	5.469	>48.65	>8.896
d	3-CH₃PhSO₂	1.8438	>100 (1.024)^a	n/d	n/d
e	4-CH₃PhSO₂	1.8438	>100^a	n/d	n/d
PH-27		0.6308	0.466	>34.73	>74.53
LZD		0.5321	<0.20	>33.73	>168.6
INH		−0.668	0.034	>100	>2941

^aConcentration that inhibited 50% growth of M. tb. (IC₅₀).