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50 values were determined using GraphPad Prism v3.02 (GraphPad Software, Inc.). Data presented is the average of at least three separate determinations. All values are given in nM and SEM given for each compound except for the less potent compounds, for which only % inhibition are reported. Full experimental details:
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50 values were determined using GraphPad Prism v3.02 (GraphPad Software, Inc.). Data presented is the average of at least three separate determinations. All values are given in nM and SEM given for each compound except for the less potent compounds, for which only % inhibition are reported. Full experimental details:. Correll C.C., Phelps P.T., Anthes J.C., Egan R.W., Umland S., and Greenfeder S. Neurosci. Lett. 370 (2004) 55
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31
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58549083592
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note
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The X-ray coordinates of compound 4 has been deposited with Cambridge Crystallographic Data Centre for small molecules (CCDC) as CCDC 708149. The ORTEP diagram of 4 (40% probability ellipsoids) is shown below:{A figure is presented}
-
-
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32
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0033136333
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The rat PK assay was run at 10 mpk using oral dosing with 20% HPBCD as vehicle. AUC was determined from 0 to 6 hours. For lead compound 24b, an additional iv dosing was performed. Reference:
-
The rat PK assay was run at 10 mpk using oral dosing with 20% HPBCD as vehicle. AUC was determined from 0 to 6 hours. For lead compound 24b, an additional iv dosing was performed. Reference:. Cox K.A., Dunn-Meynell K., Korfmacher W.A., Broske L., Nomeir A.A., Lin C.C., Cayen M.N., and Barr W.H. Drug Discov. Today 4 (1999) 232
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For a discussion on the influence of bicyclic structure on susceptibility of nucleophilic attack towards lactam carbonyls in drug design:
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37
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58549085237
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note
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-7 mol/L.
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-
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