Use of parallel-synthesis combinatorial libraries for rapid identification of potent FKBP12 inhibitors.
Using simple, inexpensive equipment, we have used solution-phase parallel synthesis to rapidly prepare hundreds of sulfonamide- and urea-containing FKBP inhibitors, resulting in rapid identification of extremely potent compounds in these series.
Choi
Chi
C
Guilford Pharmaceuticals Inc., Research Department, 6611 Tributary Street, Baltimore, MD 21224, USA.
Li
Jia-He
JH
Vaal
Mark
M
Thomas
Christine
C
Limburg
David
D
Wu
Yong-Qian
YQ
Chen
Yi
Y
Soni
Raj
R
Scott
Chad
C
Ross
Douglas T
DT
Guo
Hong
H
Howorth
Pamela
P
Valentine
Heather
H
Liang
Shi
S
Spicer
Dawn
D
Fuller
Mike
M
Steiner
Joseph
J
Hamilton
Gregory S
GS
D020650:Combinatorial Chemistry Techniques / Q000379:methods*; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D010875:Pipecolic Acids / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000494:pharmacology; D022061:Tacrolimus Binding Protein 1A / Q000037:antagonists & inhibitors*; D014508:Urea / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology
D004791:Enzyme Inhibitors; D010875:Pipecolic Acids; D013449:Sulfonamides; D014508:Urea; D022061:Tacrolimus Binding Protein 1A