Differential activity of rosiglitazone enantiomers at PPARγ

Bioorganic and Medicinal Chemistry Letters

Volumn 8, Issue 24, 1998, Pages 3657-3658

  Parks, Derek J ^a   Tomkinson, Nicholas C O ^a   Villeneuve, Manon S ^a   Blanchard, Steven G ^a   Willson, Timothy M ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR; ROSIGLITAZONE;

ARTICLE; BINDING AFFINITY; BINDING COMPETITION; DRUG ACTIVITY; ENANTIOMER; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; ISOMER; RECEPTOR BINDING;

HYPOGLYCEMIC AGENTS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; STEREOISOMERISM; THIAZOLES; THIAZOLIDINEDIONES; TRANSCRIPTION FACTORS;

EID: 0032534845     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(98)00664-7     Document Type: Article

References (12)

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7. D + 106 (c, 0.53; MeOH); 99% ee. Stereochemical assignments were made by comparison with references 5 and 6. The authors acknowledge the assistance of Nicole Doria with this separation.
8. 8. Nichols, J. S.; Parks, D. J.; Consler, T. G.; Blanchard, S. G. Anal. Biochem. 1998, 257, 112.
9. 50s were calculated ± SE, n=3.
10. 10. Consistent with this observation, both 1a and 1b show equivalent activity in cell-based reporter gene assays that require >12 h incubation with the test compound.
11. 11. Young, P. W.; Buckle, D. R.; Cantello, B. C. C.; Chapman, H.; Clapham, J. C.; Coyle, P. J.; Haigh, D.; Hindley, R. M., Holder, J. C.; Kallender, H.; Latter, A. J.; Lawrie, K. W. M.; Mossakowska, D.; Murphy, G. J.; Cox, L. R.; Smith, S. A. J. Pharmacol. Exp. Ther. 1998, 254, 751.
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