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. 2013 Feb 4;4(3):353–357. doi: 10.1021/ml300467n

Table 1. Modifications of the N-Methylpiperazine Moiety at C-2.

graphic file with name ml-2012-00467n_0008.jpg

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