Synthesis and evaluation of chiral bicyclic proline FKBP12 ligands.
As part of our ongoing program to explore novel structural classes of FKBP12 ligands, we herein wish to report a new class of FKBP12 ligands containing chiral bicyclic proline analogues. Details of the synthetic routes, together with preliminary biological activity, will be presented.
Limburg
David C
DC
Guilford Pharmaceuticals Inc., Research Department, 6611 Tributary Street, Baltimore, MD 21224, USA.
Thomas
Bert E
BE
Li
Jia-He
JH
Fuller
Mike
M
Spicer
Dawn
D
Chen
Yi
Y
Guo
Hongzhi
H
Steiner
Joseph P
JP
Hamilton
Gregory S
GS
Wu
Yong-Qian
YQ
D015632:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; D000818:Animals; D001665:Binding Sites; D001643:Bridged Bicyclo Compounds / Q000138:chemical synthesis* / Q000494:pharmacology*; D015259:Dopamine Agents; D007202:Indicators and Reagents; D008024:Ligands; D008297:Male; D051379:Mice; D008958:Models, Molecular; D008968:Molecular Conformation; D018696:Neuroprotective Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D010302:Parkinson Disease, Secondary / Q000139:chemically induced / Q000188:drug therapy; D011392:Proline / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D022061:Tacrolimus Binding Protein 1A / Q000187:drug effects*
D001643:Bridged Bicyclo Compounds; D015259:Dopamine Agents; D007202:Indicators and Reagents; D008024:Ligands; D018696:Neuroprotective Agents; D011392:Proline; D015632:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; D022061:Tacrolimus Binding Protein 1A