Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors.
The synthesis of novel [1,2,4]oxadiazoles and their structure-activity relationship (SAR) for the inhibition of tryptase and related serine proteases is presented. Elaboration of the P'-side afforded potent, selective, and orally bioavailable tryptase inhibitors.
Sperandio
David
D
Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. david.sperandio@gilead.com
Tai
Vincent W-F
VW
Lohman
Julia
J
Hirschbein
Bernie
B
Mendonca
Rohan
R
Lee
Chang-Sun
CS
Spencer
Jeffrey R
JR
Janc
James
J
Nguyen
Margaret
M
Beltman
Jerlyn
J
Sprengeler
Paul
P
Scheerens
Heleen
H
Lin
Tong
T
Liu
Liang
L
Gadre
Ashwini
A
Kellogg
Alisha
A
Green
Michael J
MJ
McGrath
Mary E
ME
D000284:Administration, Oral; D001682:Biological Availability; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D008958:Models, Molecular; D012697:Serine Endopeptidases / Q000187:drug effects*; D013329:Structure-Activity Relationship; D053802:Tryptases
D004791:Enzyme Inhibitors; D012697:Serine Endopeptidases; D053802:Tryptases