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35649024717
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note
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50s were calculated by using a log-logit plot of percent inhibition. See Ref. 2b for further details.
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18
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35648962328
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note
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4-Phenyl-piperidine-1,4-dicarboxylic acid mono-tert-butyl ester was purchased from Arch Chemicals, Inc., and 4-(4-chloro-phenyl)-piperidine-1,4-dicarboxylic acid mono-tert-butyl ester was purchased from Chem-Impex International, Inc.
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-
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20
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35648950396
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note
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i calculated via the Cheung-Prussoff equation. See Ref. 10 for further details.
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21
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14744274245
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Damiano, B.7
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22
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35648966456
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note
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2H: C, 46.58; H, 4.63; N, 6.76. Found: C, 46.25, H, 4.48; N, 6.73.
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-
-
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23
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35649027829
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note
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An optimized rat U-II homology model was constructed by using bovine rhodopsin X-ray crystal structure (PDB code 1L9H) as a template and following the same procedure described in Ref. 2b Molecular docking into the homology model was done using Glide (Schrodinger LLC, Portland, OR) with OPLS_2005 force field. Feature constraint was employed in docking, using Asp-130 as an anchor point. A basic nitrogen feature has to be fitted into the proximity of the carboxylic acid oxygen atoms.
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24
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33847109791
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Qi J., Schulingkamp R., Parry T.J., Colburn R., Stone D., Haertlein B., Minor L.K., Andrade-Gordon P., and Damiano B.P. Br. J. Pharmcol. 150 (2007) 415
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Minor, L.K.7
Andrade-Gordon, P.8
Damiano, B.P.9
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