Journal
ORGANIC LETTERS
Volume 3, Issue 25, Pages 3987-3990Publisher
AMER CHEMICAL SOC
DOI: 10.1021/ol0166909
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[GRAPHICS] 2-Aryl-2,2-difluoroacetamido-proline and pipecolate esters are high affinity FKBP12 ligands whose rotamase inhibitory activity is comparable to that seen for the corresponding ketoamides. X-ray structural studies suggest that the fluorine atoms participate in discrete interactions with the Phe36 phenyl ring and the Tyr26 hydroxyl group, with the latter resembling a moderate-to-weak hydrogen bond.
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