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Design and synthesis of potent, orally active, inhibitors of carboxypeptidase U (TAFIa) |
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| Authors: | Polla Magnus O Tottie Louise Nordén Carita Linschoten Marcel Müsil Djordje Trumpp-Kallmeyer Susanne Aukrust Inger R Ringom Rune Holm Kjetil H Neset Siren M Sandberg Marcel Thurmond John Yu Peng Hategan Georgeta Anderson Herb |
| Affiliation: | Department of Medicinal Chemistry, AstraZeneca R&D M?lndal, S-431 83 M?lndal, Sweden. magnus.polla@astrazeneca.com |
| Abstract: | A series of 3-mercapto-propionic acid derivatives that function as reversible inhibitors of carboxypeptidase U have been prepared. We present a successful design strategy using cyclic, low basicity guanidine mimetics resulting in potent, selective and bioavailable inhibitors of carboxypeptidase U (TAFIa). |
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