Literature DB >> 14980627

Design and synthesis of potent, orally active, inhibitors of carboxypeptidase U (TAFIa).

Magnus O Polla1, Louise Tottie, Carita Nordén, Marcel Linschoten, Djordje Müsil, Susanne Trumpp-Kallmeyer, Inger R Aukrust, Rune Ringom, Kjetil H Holm, Siren M Neset, Marcel Sandberg, John Thurmond, Peng Yu, Georgeta Hategan, Herb Anderson.   

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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Year:  2004        PMID: 14980627     DOI: 10.1016/j.bmc.2003.12.039

Source DB:  PubMed          Journal:  Bioorg Med Chem        ISSN: 0968-0896            Impact factor:   3.641


  8 in total

1.  Design and synthesis of potential mechanism-based inhibitors of the aminotransferase BioA involved in biotin biosynthesis.

Authors:  Ce Shi; Courtney C Aldrich
Journal:  J Org Chem       Date:  2012-07-03       Impact factor: 4.354

2.  Selective synthesis of 3-hydroxy acids from Meldrum's acids using SmI2-H2O.

Authors:  Michal Szostak; Malcolm Spain; David J Procter
Journal:  Nat Protoc       Date:  2012-04-26       Impact factor: 13.491

3.  Catalytic Asymmetric Total Synthesis of (-)-Actinophyllic Acid.

Authors:  Lingchao Cai; Kui Zhang; Ohyun Kwon
Journal:  J Am Chem Soc       Date:  2016-03-04       Impact factor: 15.419

4.  Nucleophile assisting leaving groups: a strategy for aliphatic 18F-fluorination.

Authors:  Shuiyu Lu; Salvatore D Lepore; Song Ye Li; Deboprosad Mondal; Pamela C Cohn; Anjan K Bhunia; Victor W Pike
Journal:  J Org Chem       Date:  2009-08-07       Impact factor: 4.354

Review 5.  Carboxypeptidase U (CPU, TAFIa, CPB2) in Thromboembolic Disease: What Do We Know Three Decades after Its Discovery?

Authors:  Karen Claesen; Joachim C Mertens; Dorien Leenaerts; Dirk Hendriks
Journal:  Int J Mol Sci       Date:  2021-01-17       Impact factor: 5.923

Review 6.  Samarium(ii) iodide-mediated reactions applied to natural product total synthesis.

Authors:  Majid M Heravi; Azadeh Nazari
Journal:  RSC Adv       Date:  2022-03-30       Impact factor: 3.361

7.  Syntheses of fluorooxindole and 2-fluoro-2-arylacetic acid derivatives from diethyl 2-fluoromalonate ester.

Authors:  Antal Harsanyi; Graham Sandford; Dmitri S Yufit; Judith Ak Howard
Journal:  Beilstein J Org Chem       Date:  2014-05-22       Impact factor: 2.883

8.  Structure-guided, single-point modifications in the phosphinic dipeptide structure yield highly potent and selective inhibitors of neutral aminopeptidases.

Authors:  Stamatia Vassiliou; Ewelina Węglarz-Tomczak; Łukasz Berlicki; Małgorzata Pawełczak; Bogusław Nocek; Rory Mulligan; Andrzej Joachimiak; Artur Mucha
Journal:  J Med Chem       Date:  2014-09-22       Impact factor: 7.446

  8 in total

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