title: Synthesis and evaluation of chiral bicyclic proline FKBP12 ligands.
abstract: 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.
authors.affiliation: Guilford Pharmaceuticals Inc., Research Department, 6611 Tributary Street, Baltimore, MD 21224, USA.
authors.forename: David C
authors.initials: DC
authors.lastname: Limburg
authors.forename: Bert E
authors.initials: BE
authors.lastname: Thomas
authors.forename: Jia-He
authors.initials: JH
authors.lastname: Li
authors.forename: Mike
authors.initials: M
authors.lastname: Fuller
authors.forename: Dawn
authors.initials: D
authors.lastname: Spicer
authors.forename: Yi
authors.initials: Y
authors.lastname: Chen
authors.forename: Hongzhi
authors.initials: H
authors.lastname: Guo
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Steiner
authors.forename: Gregory S
authors.initials: GS
authors.lastname: Hamilton
authors.forename: Yong-Qian
authors.initials: YQ
authors.lastname: Wu
mesh_terms: 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*
chemical_list: 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