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Ren, J.14
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Biller, S.A.26
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Zhang, H.12
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Jeon, Y.16
Seethala, R.17
Yang, W.-P.18
Ren, J.19
Zhou, M.20
Ryono, D.21
Biller, S.22
Mookhtiar, K.A.23
Wetterau, J.24
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Grover, G.11
Ma, Z.12
Moore, L.13
Seethala, R.14
Sun, W.15
Doweyko, A.M.16
Chandrasena, G.17
Sleph, P.18
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Cheng, P.T.W.20
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Wang W., Devasthale P.V., Farrelly D., Gu L., Harrity T., Cap M., Chu C., Kunselman L., Morgan N., Ponticiello R., Zebo R., Zhang L., Locke K., Lippy J., O'Malley K., Hosagrahara V., Zhang L., Kadiyala P., Chang C., Muckelbauer J., Doweyko A.M., Zahler R., Ryono D., Hariharan N., and Cheng P.T.W. Bioorg. Med. Chem. Lett. 18 (2008) 1939
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Kunselman, L.8
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Ponticiello, R.10
Zebo, R.11
Zhang, L.12
Locke, K.13
Lippy, J.14
O'Malley, K.15
Hosagrahara, V.16
Zhang, L.17
Kadiyala, P.18
Chang, C.19
Muckelbauer, J.20
Doweyko, A.M.21
Zahler, R.22
Ryono, D.23
Hariharan, N.24
Cheng, P.T.W.25
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44649174657
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Cheng, P. T. W.; Chen, S.; Devasthale, P.; Ding, C. Z.; Herpin, T. F.; Wu, S.; Zhang, H.; Wang, W.; Ye, X.-Y. WO 2004004665 A2.
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Cheng, P. T. W.; Chen, S.; Devasthale, P.; Ding, C. Z.; Herpin, T. F.; Wu, S.; Zhang, H.; Wang, W.; Ye, X.-Y. WO 2004004665 A2.
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20
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44649135746
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note
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3-(tert-Butyldimethylsilyloxy)benzylzinc chloride was prepared freshly from the corresponding benzyl chloride and activated zinc.
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24
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44649190084
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note
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Acid-mediated ester hydrolysis was chosen because our previous experience with the analogous pyrrolidine acid series (e.g. 2) had shown that base-mediated hydrolysis can result in epimerization at the carbon α to the carboxylic acid (e.g. analogs 22-25 in Scheme 3).
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25
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44649169983
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note
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Compound 27 was synthesized following the procedure in Scheme 2.
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27
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44649134207
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note
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1H COSY and HMQC. All proton and carbon assignments were also confirmed using HMBC. For example, in the HMBC spectrum, H-24 (δ 6.73) showed a correlation with C-29 (carbonyl, δ 153.2), while the benzylic protons H-22 (δ 3.36, doublet) showed connectivity with C-23 (δ 115.3), C-24 (δ 123.7), C-28 (δ 40.7), C-16 (δ 116.0), C-17 (δ 141.5), and C-18 (δ 121.9, as shown in Fig. 4). Complete analysis from this set of NMR experiments showed that the structure was unequivocally 33a rather than 34a.
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30
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33947235658
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50 values (μM) for PPARα and PPARγ were determined by calculating the amount of test ligand required for the half-maximal inhibition of the specific binding of fluorescein-labeled analog of a potent dual PPARα/γ activator to the PPARα or γ LBD, respectively. See:
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50 values (μM) for PPARα and PPARγ were determined by calculating the amount of test ligand required for the half-maximal inhibition of the specific binding of fluorescein-labeled analog of a potent dual PPARα/γ activator to the PPARα or γ LBD, respectively. See:. Seethala R., Golla R., Ma Z., Zhang H., O'Malley K., Lippy J., Cheng L., Mookhtiar K., Farrelly D., Zhang L., Hariharan N., and Cheng P.T.W. Anal. Biochem. 363 (2007) 263
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(2007)
Anal. Biochem.
, vol.363
, pp. 263
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Seethala, R.1
Golla, R.2
Ma, Z.3
Zhang, H.4
O'Malley, K.5
Lippy, J.6
Cheng, L.7
Mookhtiar, K.8
Farrelly, D.9
Zhang, L.10
Hariharan, N.11
Cheng, P.T.W.12
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31
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44649132237
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note
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50 values (μM) for PPARα or γ agonist activity were calculated as the concentration of the test ligand (μM) required for the half-maximal fold induction of HEK293 cells. The 'intrinsic activity' of a test ligand is defined as its activity at 1 μM (expressed as a percentage) relative to the activity of the primary standards at 1 μM. Also see Ref. 9a.
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