Table 16.
Compound | Reagent 58 | R | R1 | Yield of 59 (%) | Antibacterial Activity of Compounds 59 (MIC in μg/mL) | |||||
---|---|---|---|---|---|---|---|---|---|---|
BS | CT | SA | EC | ST | VC | |||||
59a | H | F | 71 | 250 | 250 | 500 | 200 | 200 | 250 | |
59b | H | Me | 83 | 250 | 100 | 250 | 500 | 500 | 250 | |
59c | Me | F | 78 | 250 | 100 | 125 | 200 | 250 | 200 | |
59d | Me | Me | 79 | 500 | 500 | 500 | 200 | 250 | 500 | |
59e | H | F | 78 | 100 | 250 | 500 | 250 | 500 | 250 | |
59f | H | Me | 72 | 200 | 500 | 100 | 250 | 250 | 200 | |
59g | Me | F | 75 | 250 | 250 | 250 | 200 | 250 | 250 | |
59h | Me | Me | 70 | 250 | 250 | 250 | 125 | 100 | 125 | |
59i | H | F | 73 | 250 | 100 | 500 | 100 | 200 | 100 | |
59j | H | Me | 83 | 200 | 250 | 500 | 125 | 100 | 250 | |
59k | Me | F | 81 | 100 | 100 | 62.5 | 200 | 125 | 125 | |
59l | Me | Me | 84 | 500 | 200 | 200 | 100 | 200 | 100 | |
59m | H | F | 75 | 200 | 100 | 500 | 200 | 250 | 200 | |
59n | H | Me | 86 | 500 | 500 | 200 | 200 | 200 | 500 | |
59o | Me | F | 70 | 125 | 500 | 500 | 125 | 100 | 100 | |
59p | Me | Me | 82 | 100 | 100 | 500 | 200 | 250 | 100 | |
59q | H | F | 68 | 250 | 500 | 250 | 100 | 125 | 250 | |
59r | H | Me | 73 | 500 | 250 | 250 | 250 | 250 | 500 | |
59s | Me | F | 75 | 250 | 250 | 250 | 62.5 | 100 | 250 | |
59t | Me | Me | 76 | 250 | 250 | 500 | 250 | 500 | 250 | |
Ampicillin a | -- | -- | -- | -- | 100 | 250 | 100 | 100 | 100 | 250 |
Norfloxacin a | -- | -- | -- | -- | 10 | 50 | 10 | 10 | 10 | 100 |
Chloramphenicol a | -- | -- | -- | -- | 50 | 50 | 50 | 50 | 50 | 50 |
Ciprofloxacin a | -- | -- | -- | -- | 50 | 100 | 25 | 25 | 25 | 50 |
BS (Bacillus subtilis), CT (Clostridium tetani), SA (Staphylococcus aureus), EC (Escherichia coli), ST (Salmonella typhi), VC (Vibrio cholerae). a Positive control for the study.