Literature DB >> 15080996

Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P(1)(') group.

Philippe G Nantermet1, James C Barrow, Stacey R Lindsley, MaryBeth Young, Shi-Shan Mao, Steven Carroll, Carolyn Bailey, Michele Bosserman, Dennis Colussi, Daniel R McMasters, Joseph P Vacca, Harold G Selnick.   

Abstract

Structural modifications of the aminopyridine P(1)(') group of imidazole acetic acid based TAFIa inhibitors led to the discovery of the aminocyclopentyl analog 28, a 1 nM TAFIa inhibitor with CLT(50) functional activity of 14 nM but without selectivity against CPB. While not as active, aminobutyl derivative 27 provided an improved 6.7-fold selectivity for TAFIa versus CPB.

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Year:  2004        PMID: 15080996     DOI: 10.1016/j.bmcl.2004.02.033

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  8 in total

1.  A diversity-oriented synthesis of 3-(2-amino-1,6-dihydro-6-oxo-pyrimidin-5-yl)propanoic esters.

Authors:  Xavier Berzosa; Sofia Pettersson; Jordi Teixidó; José I Borrell
Journal:  Mol Divers       Date:  2010-11-12       Impact factor: 2.943

Review 2.  Carboxypeptidase U (TAFIa): a new drug target for fibrinolytic therapy?

Authors:  J L Willemse; E Heylen; M E Nesheim; D F Hendriks
Journal:  J Thromb Haemost       Date:  2009-08-28       Impact factor: 5.824

3.  Concise total synthesis of (±)-actinophyllic acid.

Authors:  Brett A Granger; Ivan T Jewett; Jeffrey D Butler; Stephen F Martin
Journal:  Tetrahedron       Date:  2014-07-08       Impact factor: 2.457

4.  2-(4-Chloro-phen-yl)-4,5-diphenyl-1-(prop-2-en-1-yl)-1H-imidazole.

Authors:  Shaaban K Mohamed; Mehmet Akkurt; Adel A E Marzouk; Francisco Santoyo-Gonzalez; Mahmoud A A Elremaily
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-05-11

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

6.  2-(3,4-Dimeth-oxy-phen-yl)-4,5-diphenyl-1-(prop-2-en-1-yl)-1H-imidazole.

Authors:  Shaaban K Mohamed; Mehmet Akkurt; Frank R Fronczek; Adel A E Marzouk; Antar A Abdelhamid
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2012-09-22

7.  cis-Di-aqua-tetra-kis-(1-butyl-1H-imidazole-κN (3))nickel(II) dichloride.

Authors:  P S Kannan; A S Ganeshraja; K Rajkumar; K Anbalagan; A Subbiahpandi
Journal:  Acta Crystallogr Sect E Struct Rep Online       Date:  2013-08-17

8.  Experimental and Theoretical Analysis of Metal Complex Diffusion through Cell Monolayer.

Authors:  Katarzyna Gałczyńska; Jarosław Rachuna; Karol Ciepluch; Magdalena Kowalska; Sławomir Wąsik; Tadeusz Kosztołowicz; Katarzyna D Lewandowska; Jacek Semaniak; Krystyna Kurdziel; Michał Arabski
Journal:  Entropy (Basel)       Date:  2021-03-17       Impact factor: 2.524

  8 in total

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