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ID: ALA1130641
Journal: Bioorg Med Chem Lett
Title: 5,5-trans lactone-containing inhibitors of serine proteases: identification of a novel, acylating thrombin inhibitor.
Authors: Finch H, Pegg NA, McLaren J, Lowdon A, Bolton R, Coote SJ, Dyer U, Montana JG, Owen MR, Dowle M, Buckley D, Ross BC, Campbell C, Dix C, Mooney C, Man-Tang C, Patel C.
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.
CiteXplore: 9873654