Table 1

SARs of N-linked aryl benzothiazoles. Mean EC50 values ± S.D. and number of replicates (n) for aryl amides with the N-linked aryl benzothiazole scaffold.Embedded Image

R1R2R3XR4EC50 (μM)n
9Embedded ImageHHCHMe0.063 ± 0.0282
10Embedded ImageMeHCHH0.13 ± 0.072
11Embedded ImageHMeCHH0.17 ± 0.102
12Embedded ImageHClCHH7.96 ± 1.712
13Embedded ImageHHNH0.98 ± 0.122
14Embedded ImageHHCHMe0.080 ± 0.0183
15Embedded ImageHHCHH0.27 ± 0.032
16Embedded ImageHHCHMe0.092 ± 0.0052
17Embedded ImageHHCHH0.47 ± 0.052
18Embedded ImageMeHCHH0.481
19Embedded ImageHHCHMe0.45 ± 0.252
20Embedded ImageHHCHMe7.66 ± 2.532
21Embedded ImageHHCHMe0.084 ± 0.0142
22Embedded ImageHHCHMe1.68 ± 0.092
23Embedded ImageHHNH0.15 ± 0.012
24Embedded ImageHHNH0.38 ± 0.042