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SAR of fluorine substituted benzisothiazolones. PMI and PMM2 assay data are the mean of at least three determinations. See Experimental Section for assay details.
 | ||||
|---|---|---|---|---|
| cmpd | R | Ar | PMI IC50 (µM) |
PMM2 IC50 (µM) |
| 17 | 6-F | 2,5-di-Me-Ph | 1.0 | 7.3 |
| 18 | 6-F | 4-OMe-Ph | 3.1 | 12.9 |
| 19 | 5-F | Ph | 1.3 | >80 |
| 20 | 5-F | 2,5-di-Me-Ph | 1.9 | 31.3 |
| 21 | 5-F | 4-F-Ph | 3.6 | >80 |
| 22 | 5-F | 4-OMe-Ph | 1.0 | 9.1 |
| 23 | 5-F | 2-F-Ph | 4.3 | >20 |
| 24 | 5-F | 4-Cl-Ph | 1.8 | >20 |
| 25 | 5-F | 3-F-Ph | 8.3 | >20 |
| 26 | 6-F | 2-Me-Ph | 2.9 | >20 |
