Table 1.
Antimicrobial activities (MIC, µM) and cLogP values of analogues 17–21.
| Cmpd | cLogP a | S. a b | MRSA c | P. a d | E. c e | K. p f | A. b g | C. a h | C. n i |
|---|---|---|---|---|---|---|---|---|---|
| 17a | 5.1 | 677 | >43.3 | 677 | 677 | >43.3 | >43.3 | >43.3 | >43.3 |
| 17b | 6.0 | 200 | >41.7 | 200 | 200 | >41.7 | >41.7 | >41.7 | >41.7 |
| 17c | 6.5 | 256 | >41.0 | >256 | 256 | >41.0 | >41.0 | >41.0 | >41.0 |
| 17d | 6.9 | 50 | >40.3 | >100 | 100 | >40.3 | >40.3 | >40.3 | >40.3 |
| 17e | 7.8 | 244 | 9.72 | 608 | 608 | >38.9 | >38.9 | >38.9 | 38.9 |
| 17f | 8.7 | 25 | 0.29 | 300 | 100 | >37.6 | 0.29 | >37.6 | 0.29 |
| 18a | 4.8 | 568 | >36.3 | 568 | 568 | >36.3 | >36.3 | >36.3 | >36.3 |
| 18b | 5.7 | >200 | >35.2 | >200 | >200 | >35.2 | >35.2 | >35.2 | >35.2 |
| 18c | 6.2 | >200 | >34.7 | 200 | 200 | >34.7 | >34.7 | >34.7 | >34.7 |
| 18d | 6.6 | 107 | >34.2 | >107 | >107 | >34.2 | >34.2 | >34.2 | >34.2 |
| 18e | 7.5 | 104 | 33.2 | 518 | 518 | >33.2 | >33.2 | >33.2 | 33.2 |
| 18f | 8.4 | 3.15 | ≤0.25 | >100 | 12.5 | >32 | >32 | >32 | ≤0.25 |
| 19a | 5.1 | 34 | 43.3 | 677 | 271 | >43.3 | >43.3 | >43.3 | 21.7 |
| 19b | 6.0 | 65.2 | 41.7 | >130 | 130 | >41.7 | >41.7 | >41.7 | 20.9 |
| 19c | 6.5 | 16.0 | ≤0.32 | 32.0 | 16.0 | >41 | >41 | >41 | ≤0.32 |
| 19d | 6.9 | 7.9 | 40.3 | 126 | 126 | >40.3 | >40.3 | >40.3 | 40.3 |
| 19e | 7.8 | 30 | 1.22 | 608 | 122 | 38.9 | 38.9 | 38.9 | 4.86 |
| 19f | 8.7 | 100 | 0.294 | 300 | 300 | >37.6 | 0.294 | >37.6 | 0.294 |
| 20a | 4.8 | 57 | 18.16 | 568 | 227 | >36.3 | >36.3 | >36.3 | >36.3 |
| 20b | 5.7 | >200 | >35.2 | >200 | 50 | >35.2 | >35.2 | >35.2 | 35.2 |
| 20c | 6.2 | 25 | 2.2 | >200 | 25 | >34.7 | >34.7 | >34.7 | ≤0.27 |
| 20d | 6.6 | 13.3 | >34.2 | >107 | 107 | >34.2 | >34.2 | >34.2 | 17.1 |
| 20e | 7.5 | 12.95 | 16.6 | 518 | 104 | >33.2 | >33.2 | >33.2 | 16.6 |
| 20f | 8.4 | 3.125 | ≤0.25 | >100 | 6.3 | >32 | >32 | >32 | ≤0.25 |
| 21a | 5.7 | 300 | 0.268 | 300 | 300 | >34.3 | >34.3 | >34.3 | >34.3 |
| 21b | 6.6 | 300 | 2.08 | 300 | 300 | >33.3 | >33.3 | >33.3 | >33.3 |
| 21c | 7.1 | 200 | 0.256 | 300 | 300 | >32.8 | >32.8 | >32.8 | >32.8 |
| 21d | 7.6 | 300 | 0.506 | 300 | 300 | >32.4 | >32.4 | >32.4 | >32.4 |
| 21e | 8.5 | 300 | 0.246 | 300 | 300 | >31.5 | >31.5 | 31.5 | 15.73 |
a cLogP values calculated in DataWarrior v05.05.00 [33]; b S. aureus (ATCC 25,923 or ATCC 29213) with streptomycin (MIC 21.5 µM) and chloramphenicol (MIC 1.5–3 µM) were used as positive controls, and values are presented as the mean (n = 3); c MRSA (ATCC 43300) with vancomycin (MIC 0.7 µM) was used as a positive control, and values are presented as the mean (n = 2); d P. aeruginosa (PAO1 or ATCC 27853) with streptomycin (MIC 21.5 µM) and colistin (MIC 1 μM) were used as positive controls, and values are presented as the mean (n = 3); e E. coli (ATCC 25922) with colistin (MIC 2 µM) was used as a positive control, and values are presented as the mean (n = 2); f K. pneumoniae (ATCC 700603) with colistin (MIC 0.2 µM) was used as a positive control, and values are presented as the mean (n = 2); g A. baumannii (ATCC 19606) with colistin (MIC 0.2 µM) was used as a positive control, and values are presented as the mean (n = 2); h C. albicans (ATCC 90028) with fluconazole (MIC 0.4 µM) was used as a positive control, and values are presented as the mean (n = 2); i C. neoformans (ATCC 208821) with fluconazole (MIC 26 µM) was used as a positive control, and values are presented as the mean (n = 2).