Table 1.
Compound | AlogP | MIC (μM/μg/mL) | |||
---|---|---|---|---|---|
S. aureus | E. coli | P. aeruginosa | |||
Glyoxamide derivatives | 10a | 2.61 | 250/106 [50] | ND | ND |
10b | 3.38 | 94/47 [50] | ND | ND | |
10c | 4.26 | 24/12 [51] | ND | ND | |
10d | 5.91 | 8/4.6 | ND | ND | |
11a | 4.39 | 32/15 | ND | ND | |
11b | 5.16 | 32/18 | ND | ND | |
11c | 6.04 | 16/8.9 | ND | ND | |
11d | 7.69 | 250/158 | ND | ND | |
12a | 6.17 | 63/34 | ND | ND | |
12b | 6.94 | 250/154 | ND | ND | |
12c | 7.82 | >250/>153 | ND | ND | |
21 | 5.91 | 16/9.2 | ND | ND | |
Tertiary ammonium chloride salts | 13a | −0.89 | >250/>116 [50] | ND | ND |
13b | −0.12 | 63/34 [50] | ND | ND | |
13c | 0.76 | 16/8.6 [51] | ND | ND | |
13d | 2.41 | 16/9.8 | ND | ND | |
14a | 0.89 | 16/8.3 | ND | ND | |
14b | 1.66 | 16/9.6 | ND | ND | |
14c | 2.54 | 16/9.5 | ND | ND | |
14d | 4.18 | 125/84 | ND | ND | |
15a | 2.67 | 63/36 | ND | ND | |
15b | 3.44 | 250/163 | ND | ND | |
15c | 4.32 | >250/>163 | ND | ND | |
22 | 2.41 | 16/9.8 | ND | ND | |
Quaternary ammonium iodide salts | 16a | −1.55 | 250/142 [50] | ND | ND |
16b | −0.78 | 63/41 [50] | ND | ND | |
2, 16c | 0.10 | 16/10 [51] | 32/21 [51] | 125/80 [51] | |
16d | 1.75 | 4/2.9 | >250/>180 | >250/>180 | |
17a | 0.23 | 16/10 | ND | ND | |
17b | 1.00 | 8/5.6 | 32/22 | >250/>176 | |
17c | 1.88 | 8/5.6 | 32/22 | >250/>175 | |
17d | 3.52 | 63/48 | ND | ND | |
18a | 2.01 | 8/5.4 | >250 | >250 | |
18b | 2.78 | 125/95 | ND | ND | |
18c | 3.65 | 250/189 | ND | ND | |
23 | 1.75 | 8/5.8 | ND | ND | |
Guanidinium hydrochloride salts | 33a | −1.46 | 47/22 [50] | ND | ND |
1, 33b | −0.69 | 12/6.7 [50] | ND | ND | |
33c | 0.19 | 8/4.4 [51] | 63/35 [51] | 63/35 [51] | |
33d | 1.84 | 16/10 | ND | ND | |
34a | 0.32 | 8/4.3 | 16/8.5 | >250/>133 | |
34b | 1.09 | 16/9.8 | >250/>153 | >250/>153 | |
34c | 1.97 | 32/19 | ND | ND | |
35a | 2.10 | 250/147 | ND | ND | |
35b | 2.87 | >250/>167 | ND | ND | |
35c | 3.75 | >250/>166 | ND | ND |
ND = Not determined.