Literature DB >> 11551756

Synthesis and in vitro evaluation of a series of diketopiperazine inhibitors of plasminogen activator inhibitor-1.

A Folkes1, M B Roe, S Sohal, J Golec, R Faint, T Brooks, P Charlton.   

Abstract

We have synthesized and evaluated a series of diketopiperazine-based inhibitors of PAI-1. These studies resulted in the identification of 34 which inhibited PAI-1 in vitro with an IC(50)=0.2 microM. The synthesis and SAR of these compounds are described.

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Year:  2001        PMID： 11551756     DOI： 10.1016/s0960-894x(01)00508-x

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


  9 in total

1.  Cyclic dipeptides produced by fungus Eupenicillium brefeldianum HMP-F96 induced extracellular alkalinization and H2O 2 production in tobacco cell suspensions.

Authors:  Xiaoqi Chen; Yanhua Mou; Junhong Ling; Nan Wang; Xiao Wang; Jiangchun Hu
Journal:  World J Microbiol Biotechnol       Date:  2014-10-25       Impact factor: 3.312

2.  Novel bis-arylsulfonamides and aryl sulfonimides as inactivators of plasminogen activator inhibitor-1 (PAI-1).

Authors:  Nadine C El-Ayache; Shih-Hon Li; Mark Warnock; Daniel A Lawrence; Cory D Emal
Journal:  Bioorg Med Chem Lett       Date:  2009-12-21       Impact factor: 2.823

Review 3.  Solid-phase and microwave-assisted syntheses of 2,5-diketopiperazines: small molecules with great potential.

Authors:  Jennifer C O'Neill; Helen E Blackwell
Journal:  Comb Chem High Throughput Screen       Date:  2007-12       Impact factor: 1.339

4.  Low Molecular Weight Antagonists of Plasminogen Activator Inhibitor-1: Therapeutic Potential in Cardiovascular Disease.

Authors:  Tessa M Simone; Paul J Higgins
Journal:  Mol Med Ther       Date:  2012-08-05

5.  Chemical Antagonists of Plasminogen Activator Inhibitor-1: Mechanisms of Action and Therapeutic Potential in Vascular Disease.

Authors:  Tessa M Simone; Stephen P Higgins; Craig E Higgins; Michelle R Lennartz; Paul J Higgins
Journal:  J Mol Genet Med       Date:  2014-10

6.  Purification and synergistic antibacterial activity of arginine derived cyclic dipeptides, from Achromobacter sp. associated with a rhabditid entomopathogenic nematode against major clinically relevant biofilm forming wound bacteria.

Authors:  Indira Deepa; Sasidharan N Kumar; Ravikumar S Sreerag; Vishnu S Nath; Chellapan Mohandas
Journal:  Front Microbiol       Date:  2015-08-25       Impact factor: 5.640

Review 7.  Serpins in thrombosis, hemostasis and fibrinolysis.

Authors:  J C Rau; L M Beaulieu; J A Huntington; F C Church
Journal:  J Thromb Haemost       Date:  2007-07       Impact factor: 5.824

Review 8.  Cyclodipeptides: An Overview of Their Biosynthesis and Biological Activity.

Authors:  Awdhesh Kumar Mishra; Jaehyuk Choi; Seong-Jin Choi; Kwang-Hyun Baek
Journal:  Molecules       Date:  2017-10-23       Impact factor: 4.411

9.  Design and synthesis of novel N-benzylidenesulfonohydrazide inhibitors of MurC and MurD as potential antibacterial agents.

Authors:  Rok Frlan; Andreja Kovac; Didier Blanot; Stanislav Gobec; Slavko Pecar; Ales Obreza
Journal:  Molecules       Date:  2008-01-11       Impact factor: 4.411
  9 in total

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