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Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors |
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| Authors: | Sutton James C Bolton Scott A Davis Malcolm E Hartl Karen S Jacobson Bruce Mathur Arvind Ogletree Martin L Slusarchyk William A Zahler Robert Seiler Steven M Bisacchi Gregory S |
| Institution: | The Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA. james.sutton@bms.com |
| Abstract: | A series of nonguanidine N1-activated C4-carboxy azetidinone tryptase inhibitors was prepared by solid-phase methodology to quickly assess the SAR associated with distal functionality on the N1-activating group. From these studies, potent inhibitors with improved specificity were discovered. |
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