Table 1.
Structures and activities of analogs 14.
Cmpd | R | mGluR5a IC50 (μM) | % Glu Maxb |
---|---|---|---|
10 |
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1.54 | 2.64 |
14a |
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1.18 | 2.69 |
14b |
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>30 | ND |
14c |
![]() |
5.02 | 2.39 |
14d |
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>10 | 56.2 |
14e |
![]() |
5.24 | 4.23 |
14f |
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>10 | 52.1 |
14g |
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>30 | ND |
14h |
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>10 | 26.1 |
14i |
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0.82 | 1.12 |
14j |
![]() |
>10 | 40.6 |
IC50s are average of three determinations.
Determined at 30 μM test compound. ND, not determined.