Table 13.
Three-component synthesis of pyrazolo-quinolines 51 and their in vitro antibacterial activity (MIC) against six bacterial strains.
| ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Compound | R | R1 | R2 | Yield of 51 (%) | Antibacterial Activity of Compounds 51 (MIC in μg/mL) | |||||
| SP | BS | CT | EC | ST | VC | |||||
| 51a | 4-F | CN | Cl | 81 | 500 | 500 | 250 | 100 | 250 | 250 |
| 51b | 4-F | CO2Et | Cl | 79 | 100 | 500 | 62.5 | 200 | 500 | 200 |
| 51c | 4-F | CONH2 | Cl | 73 | 200 | 200 | 500 | 250 | 200 | 200 |
| 51d | 4-F | CN | Me | 84 | 62.5 | 250 | 125 | 200 | 200 | 1000 |
| 51e | 4-F | CO2Et | Me | 76 | 500 | 250 | 1000 | 250 | 250 | 1000 |
| 51f | 4-CF3 | CN | Me | 72 | 500 | 500 | 500 | 250 | 100 | 62.5 |
| 51g | 4-CF3 | CO2Et | Me | 80 | 100 | 100 | 500 | 500 | 200 | 500 |
| 51h | 2,4-F | CN | Me | 79 | 100 | 62.5 | 100 | 100 | 500 | 500 |
| 51i | 2,4-F | CO2Et | Me | 73 | 200 | 500 | 250 | 500 | 100 | 100 |
| 51j | 2,4-F | CN | Cl | 75 | 500 | 500 | 200 | 100 | 200 | 200 |
| 51k | 2,4-F | CO2Et | Cl | 78 | 100 | 1000 | 250 | 200 | 200 | 100 |
| 51l | 2,4-F | CONH2 | Cl | 81 | 500 | 500 | 200 | 500 | 500 | 500 |
| 51m | 4-F | CN | F | 83 | 200 | 100 | 200 | 62.5 | 100 | 500 |
| 51n | 4-F | CO2Et | F | 71 | 500 | 100 | 500 | 100 | 200 | 500 |
| 51o | CF3 | CN | F | 72 | 200 | 200 | 62.5 | 62.5 | 100 | 100 |
| 51p | CF3 | CO2Et | F | 77 | 500 | 1000 | 200 | 500 | 500 | 100 |
| Ampicillin a | -- | -- | -- | -- | 100 | 250 | 250 | 100 | 100 | 100 |
| Norfloxacin a | -- | -- | -- | -- | 10 | 100 | 50 | 10 | 10 | 10 |
| Chloramphenicol a | -- | -- | -- | -- | 50 | 50 | 50 | 50 | 50 | 50 |
| Ciprofloxacin a | -- | -- | -- | -- | 25 | 50 | 100 | 25 | 25 | 25 |
SP (Streptococcus pneumoniae), BS (Bacillus subtilis), CT (Clostridium tetani), EC (Escherichia coli), ST (Salmonella typhi), VC (Vibrio cholerae). a Positive control for the study.