Table 1. Modifications of the N-Methylpiperazine Moiety at C-2.
no. | R1 (2° amine) | Kdis (μM) |
---|---|---|
2 | 1-methylpiperazine | 6.9 ± 1.5 |
4 | F | >20 |
5 | 1,2-dimethylpiperazine | 4.7 ± 0.8 |
6 | 1-methyl-1,4-diazepane | 7.0 ± 1.1 |
7 | morpholine | >20 |
8 | piperidine | >20 |
9 | 1-ethylpiperazine | >20 |
10 | N1,1-dimethylpyrrolidin-3-amine | 15.8 ± 2.0 |
11 | N1,1-dimethylpiperidin-4-amine | >20 |
13 | piperazine | >20 |
15 | pyrrolidin-3-amine | >20 |
17 | piperidin-4-amine | >20 |
18 | N1,1,2-trimethylethane-1,2-diamine | >20 |