900515-72-2Relevant academic research and scientific papers
Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors
Palmer, James T.,Rydzewski, Robert M.,Mendonca, Rohan V.,Sperandio, David,Spencer, Jeffrey R.,Hirschbein, Bernard L.,Lohman, Julia,Beltman, Jeri,Nguyen, Margaret,Liu, Liang
, p. 3434 - 3439 (2007/10/03)
Using a scaleable, directed library approach based on orthogonally protected advanced intermediates, we have prepared a series of potent keto-1,2,4-oxadiazoles designed to explore the P2 binding pocket of human mast cell tryptase, while buildin
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.
