Table 2. PDE11A4 Inhibitiona.
cpd | amine | R1 | R2 | R3 | % inhib @ 500 nM | IC50 (nM) |
---|---|---|---|---|---|---|
9a | diethyl | 2-thiophenyl | CH3 | H | 580 | |
9b | pyrrolidinyl | 2-thiophenyl | CH3 | H | 0 | |
9c | azetidinyl | 2-thiophenyl | CH3 | H | 0 | |
9d | morpholinyl | 2-thiophenyl | CH3 | H | 0 | |
9e | N-Me-piperazinyl | 2-thiophenyl | CH3 | H | 0 | |
11 | diethyl | H | CH3 | H | 0 | |
12 | diethyl | CN | CH3 | H | 0 | |
13 | diethyl | pyrrolidinyl | CH3 | H | 0 | |
14a | diethyl | 2-thiazolyl | CH3 | H | 890 | |
14b | diethyl | N-Me-5-pyrazolyl | CH3 | H | 53 | |
14c | diethyl | N-Et-5-pyrazolyl | CH3 | H | 61 | |
14d | diethyl | N-iPr-5-pyrazolyl | CH3 | H | 50 | |
14e | diethyl | N-Me-3-pyrazolyl | CH3 | H | 19 | |
14f | diethyl | N-Me-4-pyrazolyl | CH3 | H | 66 | |
14g | diethyl | NH-5-pyrazolyl | CH3 | H | 21 | |
14h | Piperidinyl | N-Me-5-pyrazolyl | CH3 | H | 4800 | |
14i | t-Bu | N-Me-5-pyrazolyl | CH3 | H | 22 | |
14j | Me-n-propyl | N-Me-5-pyrazolyl | CH3 | H | 630 | |
14k | Me-Et | N-Me-5-pyrazolyl | CH3 | H | 500 | |
15 | diethyl | 2-Me-3,4-oxadiazolyl | CH3 | H | 0 | |
18a | diethyl | N-Et-5-pyrazolyl | CH3 | 2-F | 62 | |
18b | diethyl | N-Me-5-pyrazolyl | CH3 | 3-F | 65 | |
18c | diethyl | N-Me-5-pyrazolyl | CH3 | 4-F | 91 | |
18d | diethyl | N-Me-5-pyrazolyl | CH3 | 2-Cl | 51 | |
18e | diethyl | N-Me-5-pyrazolyl | CH3 | 4-Cl | 51 | |
20a | diethyl | N-Et-5-pyrazolyl | H | H | 270 | |
20b | diethyl | N-Et-5-pyrazolyl | H | 4-F | 31 | |
23a | diethyl | N-Et-5-pyrazolyl | CF3 | H | 81 | |
23b | diethyl | N-Me-5-pyrazolyl | CHF2 | H | 12 | |
25 | CD3CD2 | N-Me-5-pyrazolyl | CHF2 | H | 16 | |
1 | 25 |
IC50 values represent average of three independent determinations.