Table 1.
Compound | R1 | R2 | R3 | R4 | R5 | R6 | R7 | MIC50 | MIC90 |
---|---|---|---|---|---|---|---|---|---|
3a | OH | H | Cl | H | CH3 | H | H | >1 μM | >1 μM |
3b | OH | H | Cl | H | Br | H | H | 750-500 nM | 1 μM–750 nM |
3c | OH | H | Cl | H | CH2CH3 | H | H | 500-250 nM | 750-500 nM |
3d | OH | H | Cl | H | C≡CH | H | H | >1 μM | >1 μM |
3e | OH | H | Cl | H | CH=CH2 | H | H | 500-250 nM | 1 μM–750 nM |
3f | OH | H | Cl | H | CF3 | H | H | 500-250 nM | 500-250 nM |
3g | OH | H | Cl | H | CN | H | H | >1 μM | >1 μM |
3h | OH | H | Cl | H | F | H | H | 570-500 nM | 1 μM–750 nM |
3i | OH | H | Cl | H | C(CH3)3 | H | H | 16-8 nM | 31-16 nM |
3j | OH | H | Cl | H | CF3 | H | CF3 | 31-16 nM | 250-125 nM |
3k | OH | H | H | Cl | H | NO2 | H | >1 μM | >1 μM |
3l | OH | H | Cl | H | CH2Ph | H | H | 1 μM–750 nM | 1 μM–750 nM |
3m | OH | H | CH3 | Cl | H | NO2 | H | 500-250 nM | 500-250 nM |
3n | OH | H | Cl | H | Cl | H | Cl | 500-250 nM | 500-250 nM |
3o | OH | H | Cl | H | F | H | F | >1 μM | >1 μM |
3p | OH | H | Cl | F | H | Cl | H | 750-500 nM | 750-500 nM |
3q | OH | H | Cl | OCH3 | OCH3 | OCH3 | H | >1 μM | >1 μM |
3r | OH | H | Cl | Cl | H | H | CN | 750-500 nM | 1 μM–750 nM |
3s | OH | H | Cl | H | CH3 | H | CH3 | >1 μM | >1 μM |
3t | OH | H | Cl | H | C≡CH | F | H | >1 μM | >1 μM |
3u | OH | H | Cl | H | OCH2CH3 | H | H | >1 μM | >1 μM |
3v | OH | H | Cl | H | OCH3 | OCH3 | H | >1 μM | >1 μM |
3w | OH | H | Cl | H | OCH(CH3)2 | H | H | >1 μM | >1 μM |
3x | OH | H | Cl | H | OCH3 | H | CH3 | >1 μM | >1 μM |
3y | OH | H | Cl | H | OPh | H | H | >1 μM | >1 μM |
3z | OH | H | Cl | H | OCH(CF3)2 | H | H | >1 μM | >1 μM |
3aa | OH | I | I | H | Cl | H | H | >1 μM | >1 μM |
3ab | OH | H | Cl | H | OCH2CH2O | H | >1 μM | >1 μM | |
3ac | OH | H | F | H | OCH2CH3 | H | H | >1 μM | >1 μM |
4 | OH | H | Cl | Cl | H | NO2 | H | 250-200 nM | 250-200 nM |
5 | OH | H | Cl | Cl | H | NH2 | H | >1 μM | >1 μM |
7a | PhC(=O)O | H | Cl | Cl | H | NO2 | H | 125-61 nM | 250-125 nM |
7b | H | Cl | Cl | H | NO2 | H | >1 μM | >1 μM | |
7c | H | Cl | Cl | H | NO2 | H | >1 μM | >1 μM | |
7d | H | Cl | Cl | H | NO2 | H | 750-500 nM | 1 μM–750 nM | |
10a | CH3O | H | F | H | CH3 | H | H | >1 μM | >1 μM |
10b | CH3O | H | F | H | OCH3 | H | H | >1 μM | >1 μM |
14a | H | Cl | Cl | H | NO2 | H | 31-16 nM | 250-125 nM | |
14b | H | Cl | H | CF3 | H | CF3 | 250-125 nM | 250-125 nM |