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. 2012 Feb 7;7(2):e29434. doi: 10.1371/journal.pone.0029434

Table 2. Evaluation of antibacterial and cytotoxicity activity of propargyl-linked antifolates.

Cmpd # MICMRSAa MICMRSAb+FCS MICS.pyogenes MICS. pyogenes+FCSc IC50MCF-10(µM) IC50 HepG2(µM) Selectivityd MRSA SelectivityS. pyogenes
1 5.76 (16) ND 0.097 (0.25) ND 47 ND 3 188
2 0.71 (2) ND 0.024 (0.064) ND 55 ND 28 859
7 0.18 (1) ND 0.006 (0.016) ND 67 ND 67 4,187
8 0.66 (2) 5.2 (16) 0.66 (2) 2.6 (8) 32 ND 16 16
9 0.18 (0.5) 1.4 (4) 0.18 (0.5) 0.72 (2) 199 ND 398 398
10 0.72 (2) 11.4 (32) 0.18 (0.5) 5.7 (16) 38 94 19 76
11 0.74 (2) 11.9 (32) 0.74 (2) 6 (16) 54 77 27 27
24 0.04 (0.125) 0.09 (0.25) 0.04 (0.125) 0.09 (0.25) 220 233 1,760 1,760
25 0.09 (0.5) ND 0.012 (0.032) ND 85 171 170 2,656
26 0.02 (0.064) 0.09 (0.25) 0.04 (0.125) 0.09 (0.25) 217 199 3,391 1,736
27 0.04 (0.125) 0.09 (0.25) 0.04 (0.125) 0.09 (0.25) 409 465 3,272 3,272
28 0.08 (0.25) 0.16 (0.5) 0.04 (0.125) 0.09 (0.25) 475 >500 1,900 3,800
31 1.5 (4) 2.94 (8) 2.94 (8) 2.94 (8) 462 494 116 58
36 0.041 (0.125) ND 0.08 (0.25) ND >500 >500 >4,000 >2,000
37 0.16 (0.5) 0.16 (0.5) 0.16 (0.5) 0.16 (0.5) >500 ND >1,000 >1,000
TMP 0.14 (0.5) 0.14 (0.5) 0.58 (2) 0.58 (2) ND ND ND ND
a

MIC values for MRSA and S. pyogenes are reported in µg/mL (µM).

b

MIC values for MRSA in the presence of 10% fetal calf serum (FCS) in µg/mL (µM).

c

MIC values for S. pyogenes in the presence of 10% FCS in µg/mL (µM).

d

Selectivity values are calculated as IC50 (MCF10)/MIC (pathogen), both values in µM. ND: not determined.