908351-64-4Relevant academic research and scientific papers
Design of novel, potent, and selective human β-tryptase inhibitors based on α-keto-[1,2,4]-oxadiazoles
Lee, Chang-Sun,Liu, Weili,Sprengeler, Paul A.,Somoza, John R.,Janc, James W.,Sperandio, David,Spencer, Jeffrey R.,Green, Michael J.,McGrath, Mary E.
, p. 4036 - 4040 (2006)
A series of novel α-keto-[1,2,4]-oxadiazoles has been synthesized as human tryptase inhibitors for evaluation as a new class of anti-asthmatic agent. The inhibitor design is focused on using a prime-side hydrophobic pocket and the S2 pocket of β-tryptase
Novel, potent, selective, and orally bioavailable human βII-tryptase inhibitors
Sperandio, David,Tai, Vincent W.-F.,Lohman, Julia,Hirschbein, Bernie,Mendonca, Rohan,Lee, Chang-Sun,Spencer, Jeffrey R.,Janc, James,Nguyen, Margaret,Beltman, Jerlyn,Sprengeler, Paul,Scheerens, Heleen,Lin, Tong,Liu, Liang,Gadre, Ashwini,Kellogg, Alisha,Green, Michael J.,McGrath, Mary E.
, p. 4085 - 4089 (2007/10/03)
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.
