5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor |
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| Authors: | H Finch NA Pegg J McLaren A Lowdon R Bolton SJ Coote U Dyer JG Montana MR Owen M Dowle D Buckley BC Ross C Campbell C Dix C Mooney C Man-Tang C Patel |
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| Affiliation: | Department of Medicinal Chemistry, GlaxoWellcome Research and Development, Stevenage, Herts., U.K. hf3736@glaxowellcome.co.uk |
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| Abstract: | Synthesis of a variety of 5,5-trans fused lactones, related to compounds found in extracts of Lantana camara, has provided a series of novel acylating inhibitors of human thrombin, trypsin, chymotrypsin and human leucocyte elastase. The most effective thrombin inhibitor is 7 with an IC50 of 130 nM and a Kobs/[1] of 4,000 M-1 s-1. |
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