Design and synthesis of selective keto-1,2,4-oxadiazole-based tryptase inhibitors |
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| Authors: | 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 |
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| Institution: | Celera Genomics, 180 Kimball Way, South San Francisco, CA 94080, USA. jpalmer@rigel.com |
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| Abstract: | 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 P(2) binding pocket of human mast cell tryptase, while building in a high degree of selectivity over human trypsin and other serine proteases. |
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