TABLE 1.
Chemical structure, convulsant doses, molecular weights, and partition coefficient values of 6-desfluoroquinolone derivatives tested in ICR mice
| Compound | R6 | R7 | CD50a (95% confidence interval)
|
Mol wt | clog Pb | |
|---|---|---|---|---|---|---|
| μg/g | nmol/g | |||||
| MF-5128 | NH2 |  |
55.3 (29.9–102.1) | 128.8 | 429.35 | −0.695 |
| MF-5137 | NH2 | 37.2 (25.3–49.3) | 95.5 | 389.45 | 3.305 | |
| MF-5138 | NH2 | 50.8 (33.7–76.6) | 133.7 | 379.84 | 0.951 | |
| MF-5140 | NH2 | 35.1 (18.7–65.9) | 89.1 | 393.87 | 0.508 | |
| MF-5143 | NH2 | 40.2 (12.5–129.3) | 106.4 | 377.87 | 2.595 | |
| MF-5142 | NH2 | 52.8 (33.2–84.0) | 134.7 | 391.90 | 3.114 | |
| MF-5158 | NH2 | 46.7 (30.6–71.2) | 125.7 | 371.44 | 1.989 | |
| MF-5184 | H | 10.1 (5.3–19.2) | 27.0 | 377.44 | 4.373 | |
| MF-5187 | H | 16.3 (8.6–30.7) | 47.6 | 342.39 | 1.341 | |
| MF-5181 | H | 30.5 (15.7–59.2) | 93.4 | 326.40 | 3.663 | |
| MF-5191 | H | 43.3 (30.4–61.7) | 127.2 | 340.42 | 3.947 | |
| MF-5189 | H | 28.5 (21.6–37.6) | 73.6 | 387.18 | −0.820 | |