Table 1.
MIC values in μg/mL and (μM)a for compounds 3A,B, 4A,C-H, 7Aa-Ag, and 8Aa against various bacterial strains.
| Gram-positive | Gram-negative | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| Cpd | A (Bsu) | B (Lmo) | C (MRSA) | D (VRE) | E (Aba) | F (Ecl) | G (Eco) | H (Kpn) | I (Pae) | J (Sen) | K (Msm) |
| AMK | 3.0-12.2 (3.9-15.6) | 3.0 (3.9) | 24.5 (31.3) | 97.7 (125) | 24.5 (31.3) | 48.9 (62.5) | 24.5 (31.3) | 24.5 (31.3) | 48.9 (62.5) | 3.0-6.1 (3.9-7.8) | 12.2 (15.6) |
| AMP | >92.8 (>250) | 92.8 (250) | 92.8 (250) | 92.8 (250) | >92.8 (>250) | >92.8 (>250) | >92.8 (>250) | >92.8 (>250) | >92.8 (>250) | 92.8 (250) | >92.8 (>250) |
| OFX | ≤0.2 (≤0.5) | 0.4 (1.0) | 0.4 (1.0) | 2.8 (7.8) | ≤0.2 (≤0.5) | ≤0.2 (≤0.5) | 1.4-2.8 (3.9-7.8) | 5.6-11.3 (15.6-31.3) | 1.4 (3.9) | 5.6-11.3 (15.6-31.3) | 5.6 (15.6) |
| 3A | >198 (>500) | 0.4 (1.0) | 1.5 (3.9) | 0.8 (2.0) | >198 (>500) | >198 (>500) | >198 (>500) | >198 (>500) | >198 (>500) | >198 (>500) | >198 (>500) |
| 3B | >198 (>500) | 0.4 (1.0) | 1.5 (3.9) | 1.5 (3.9) | >198 (>500) | >198 (>500) | >198 (>500) | >198 (>500) | >198 (>500) | >198 (>500) | 0.4 (1.0) |
| 4A | >212 (>500) | >212 (>500) | >212 (>500) | >212 (>500) | >212 (>500) | 52.9 (125) | 26.5 (62.5) | 6.6 (15.6) | 0.8 (2.0) | >212 (>500) | >212 (>500) |
| 4C | >219 (>500) | 1.7 (3.9) | 1.7 (3.9) | 0.9 (2.0) | >219 (>500) | >219 (>500) | >219 (>500) | >219 (>500) | >219 (>500) | >219 (>500) | 0.9 (2.0) |
| 4D | >226 (>500) | 0.5 (1.0) | 0.5-0.9 (1.0-2.0) | 0.5 (1.0) | >226 (>500) | >226 (>500) | >226 (>500) | >226 (>500) | >226 (>500) | >226 (>500) | 0.5 (1.0) |
| 4E | 54.9 (125) | 27.5 (62.5) | 54.9 (125) | 1.7 (3.9) | 27.5 (62.5) | 110 (250) | 54.9 (125) | 27.5 (62.5) | 27.5 (62.5) | 54.9 (125) | 54.9-110 (125-250) |
| 4F | 3.4 (7.8) | <0.2 (<0.5) | 0.4-0.9 (1.0-2.0) | 0.4 (1.0) | 218 (500) | 218 (500) | 218 (500) | 13.6-27.2 (31.3-62.5) | 0.4-0.9 (1.0-2.0) | 1.7 (3.9) | 0.4 (1.0) |
| 4G | 86.8 (250) | 86.8 (250) | >173 (>500) | 43.4 (125) | 173 (500) | >173 (>500) | >173 (>500) | 173 (500) | 86.8 (250) | 86.8-173 (250-500) | >173 (>500) |
| 4H | 86.8 (250) | 86.8 (250) | >173 (>500) | 43.4 (125) | >173 (>500) | >173 (>500) | >173 (>500) | >173 (>500) | 173 (500) | 21.7-86.8 (62.5-250) | 5.4 (15.6) |
| 7Aa | >215 (>500) | 0.4-0.9 (1.0-2.0) | 0.9 (2.0) | 0.9 (2.0) | >215 (>500) | >215 (>500) | >215 (>500) | >215 (>500) | >215 (>500) | >215 (>500) | 1.7 (3.9) |
| 7Ab | >235 (>500) | 0.9 (2.0) | 0.9 (2.0) | 0.9 (2.0) | >235 (>500) | >235 (>500) | >235 (>500) | >235 (>500) | >235 (>500) | >235 (>500) | 1.8 (3.9) |
| 7Ac | >205 (>500) | 0.8 (2.0) | 3.2 (7.8) | 1.6 (3.9) | >205 (>500) | >205 (>500) | >205 (>500) | >205 (>500) | >205 (>500) | >205 (>500) | 1.6 (3.9) |
| 7Ad | >214 (>500) | 1.7 (3.9) | 3.3 (7.8) | 1.7 (3.9) | >214 (>500) | >214 (>500) | >214 (>500) | >214 (>500) | >214 (>500) | >214 (>500) | 1.7 (3.9) |
| 7Ae | 13.1 (31.3) | 3.3 (7.8) | 6.5 (15.6) | 0.8-1.6 (2.0-3.9) | 6.5-13.1 (15.6-31.3) | 209 (500) | 26.1-52.2 (62.5-125) | 6.5-13.1 (15.6-31.3) | 13.1-26.1 (31.3-62.5) | 6.5 (15.6) | 6.5-13.1 (15.6-31.3) |
| 7Af | >214 (>500) | 0.9-1.7 (2.0-3.9) | 1.7 (3.9) | 1.7 (3.9) | >214 (>500) | >214 (>500) | >214 (>500) | >214 (>500) | >214 (>500) | >214 (>500) | 0.9-1.7 (2.0-3.9) |
| 7Ag | >231 (>500) | 3.6 (7.8) | 3.6 (7.8) | 3.6 (7.8) | >231 (>500) | >231 (>500) | >231 (>500) | >231 (>500) | >231 (>500) | >231 (>500) | 1.8 (3.9) |
| 8Aa | 26.6-53.3 (62.5-125) | 26.6-53.3 (62.5-125) | 53.3 (125) | 1.7 (3.9) | 26.6 (62.5) | 213 (500) | 213 (500) | 26.6-53.3 (62.5-125) | 213 (500) | 26.3-53.3 (62.5-125) | 213 (500) |
These antibacterial MIC values were determined originally in μM using a range of 0.5 to 500 μM. These values are presented into parentheses. The values in μg/mL are presented for comparison with the antifungal MIC values, which were determined originally in μg/mL.
Gram-positive: A (Bsu) = B. subtilis 168, B (Lmo) = L. monocytogenes ATCC 19115, C = MRSA, D = VRE.
Gram-negative: E (Aba) = A. baumannii ATCC 19606, F (Ecl) = E. cloacae ATCC 13047, G (Eco) = E. coli MC1061, H (Kpn) = K. pneumoniae ATCC 27736, I (Pae) = P. aeruginosa ATCC 27853, J (Sen) = S. enterica ATCC 14028.
Mycobacterial: K (Msm) = M. smegmatis MC2-155. Note: All strains without an ATCC number are either clinical isolates or obtained from a different source than ATCC (source provided in supporting information).
Control antibiotics: AMK = amikacin, AMP = ampicillin, OFX = ofloxacin.