Novel, potent, selective, and orally bioavailable human betaII-tryptase inhibitors |
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| Authors: | 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 |
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| Affiliation: | Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. david.sperandio@gilead.com |
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| Abstract: | 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. |
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