title: Solid-phase synthesis of FKBP12 inhibitors: N-sulfonyl and N-carbamoylprolyl/pipecolyl amides.
abstract: In parallel with our work on solution-phase parallel synthesis of ligands for the rotamase enzyme FKBP12, we herein report a methodology for the solid-phase synthesis of two classes of inhibitor, N-sulfonyl and N-carbamoylprolyl and pipecolyl amides along with their in vitro/in vivo biological results.
authors: Guilford Pharmaceuticals Inc., Research Department, 6611 Tributary Street, 21224, Baltimore, MD, USA
authors: Ling
authors: L
authors: Wei
authors: Yon- Qian
authors: Y
authors: Wu
authors: Douglas E
authors: DE
authors: Wilkinson
authors: Yi
authors: Y
authors: Chen
authors: Raj
authors: R
authors: Soni
authors: Chad
authors: C
authors: Scott
authors: Douglas T
authors: DT
authors: Ross
authors: Hong
authors: H
authors: Guo
authors: Pamela
authors: P
authors: Howorth
authors: Heather
authors: H
authors: Valentine
authors: Shi
authors: S
authors: Liang
authors: Dawn
authors: D
authors: Spicer
authors: Mike
authors: M
authors: Fuller
authors: Joseph
authors: J
authors: Steiner
authors: Gregory S
authors: GS
authors: Hamilton
mesh_terms: D015632:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; D000818:Animals; D002219:Carbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D020734:Parkinsonian Disorders / Q000139:chemically induced / Q000201:enzymology; D010875:Pipecolic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013451:Sulfonic Acids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D022021:Tacrolimus Binding Proteins / Q000037:antagonists & inhibitors*
chemical_list: D002219:Carbamates; D004791:Enzyme Inhibitors; D010875:Pipecolic Acids; D013451:Sulfonic Acids; D015632:1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine; D022021:Tacrolimus Binding Proteins