Table 5. Antibacterial Activities (μM) for Selected Thienopyrimidinone Analogues.
15 |
23 |
24 |
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pathogen | MIC50a | MIC90a | MBC99.9b | MIC50 | MIC90 | MBC99.9 | MIC50 | MIC90 | MBC99.9 | |
Gram-negative | P. aeruginosa | NAc | NA | NA | NA | NA | NA | NA | NA | NA |
A. baumannii | 62 | 95 | >100 | >100 | >100 | >100 | 75 | 99 | >100 | |
K. pneumoniae | NA | NA | NA | NA | NA | NA | NA | NA | NA | |
S. enteritidis | NA | NA | NA | NA | NA | NA | >100 | >100 | >100 | |
E. coli | NA | NA | NA | NA | NA | NA | NA | NA | NA | |
Gram-positive | S. aureus | 31 | 36 | 54 | 6 | 8.5 | 34 | 5 | 8.5 | 34 |
E. faecalis | NA | NA | NA | NA | NA | NA | NA | NA | NA | |
S. pneumoniae | 60 | 73 | >100 | 34 | 56 | >100 | 62 | 74 | >100 | |
mycobacteria | M. smegmatis | 58 | 72 | >100 | 13 | 18 | 36 | 17 | 23 | 69 |
M. tuberculosis | 78 | >100d | >100 | 22 | 43 | 75 | 44 | 88 | nde |
MIC50 and MIC90 represent hit concentrations inhibiting growth by 50% and 90%, respectively.
MBC99.9 represents hit concentrations kill bacteria by 99.9%.
NA = no bacterial activity.
Denotes detectable growth inhibition or bactericidal activity but less than 50% for MIC50, less than 90% for MIC90, and less than 99.9% for MBC99.9.
nd = not determined.