Literature DB >> 11909718

Design, synthesis and in vitro evaluation of potent, novel, small molecule inhibitors of plasminogen activator inhibitor-1.

Adrian Folkes1, S David Brown, Lynne E Canne, Jocelyn Chan, Erin Engelhardt, Sergey Epshteyn, Richard Faint, Julian Golec, Art Hanel, Patrick Kearney, James W Leahy, Morrison Mac, David Matthews, Michael P Prisbylla, Jason Sanderson, Reyna J Simon, Zerom Tesfai, Nigel Vicker, Shouming Wang, Robert R Webb, Peter Charlton.   

Abstract

We have synthesized and evaluated a series of tetramic acid-based and hydroxyquinolinone-based inhibitors of plasminogen activator inhibitor-1 (PAI-1). These studies resulted in the identification of several compounds which showed excellent potency against PAI-1. The design, synthesis and SAR of these compounds are described.

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Year:  2002        PMID： 11909718     DOI： 10.1016/s0960-894x(02)00078-1

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


  6 in total

1.  Characterization of a novel class of polyphenolic inhibitors of plasminogen activator inhibitor-1.

Authors:  Jacqueline M Cale; Shih-Hon Li; Mark Warnock; Enming J Su; Paul R North; Karen L Sanders; Maria M Puscau; Cory D Emal; Daniel A Lawrence
Journal:  J Biol Chem       Date:  2010-01-08       Impact factor: 5.157

2.  Deleterious effects of lack of cardiac PAI-1 after coronary occlusion in mice and their pathophysiologic determinants.

Authors:  A K M Tarikuz Zaman; Satoshi Fujii; David J Schneider; Douglas J Taatjes; H Roger Lijnen; Burton E Sobel
Journal:  Histochem Cell Biol       Date:  2007-06-19       Impact factor: 4.304

Review 3.  Angiotensin II and progressive renal insufficiency.

Authors:  Jens Gaedeke; Nancy A Noble; Wayne A Border
Journal:  Curr Hypertens Rep       Date:  2002-10       Impact factor: 5.369

4.  Diabetes-associated dysregulated cytokines and cancer.

Authors:  Yong Wu; Yanjun Liu; Yunzhou Dong; Jay Vadgama
Journal:  Integr Cancer Sci Ther       Date:  2016-02-15

5.  Peptide-guided functionalization and macrocyclization of bioactive peptidosulfonamides by Pd(II)-catalyzed late-stage C-H activation.

Authors:  Jian Tang; Hongfei Chen; Yadong He; Wangjian Sheng; Qingqing Bai; Huan Wang
Journal:  Nat Commun       Date:  2018-08-23       Impact factor: 14.919

6.  Design, synthesis and microbiological evaluation of ampicillin-tetramic acid hybrid antibiotics.

Authors:  Philip T Cherian; Aditi Deshpande; Martin N Cheramie; David F Bruhn; Julian G Hurdle; Richard E Lee
Journal:  J Antibiot (Tokyo)       Date:  2016-05-18       Impact factor: 2.649
  6 in total

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