Literature DB >> 15896956

Synthesis of a small library of diketopiperazines as potential inhibitors of calpain.

Yibin Zeng1, Qingshan Li, Robert P Hanzlik, Jeffrey Aubé.   

Abstract

A small library of 2,5-diketopiperazines based on previously reported calpain inhibitors was synthesized. In addition, a concise total synthesis of the structurally related natural product phevalin (2) was accomplished. Despite literature reports that some of the compounds prepared were calpain inhibitors, none of the library members were found to have significant activity against recombinant human calpain I.

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Year:  2005        PMID： 15896956     DOI： 10.1016/j.bmcl.2005.04.031

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


  6 in total

1.  Calcium-dependent proteolytic activity of a cysteine protease caldonopain is detected during Leishmania infection.

Authors:  Runu Dey; Jharna Bhattacharya; Salil C Datta
Journal:  Mol Cell Biochem       Date:  2006-01       Impact factor: 3.396

2.  Aureusimines in Staphylococcus aureus are not involved in virulence.

Authors:  Fei Sun; Hoonsik Cho; Do-Won Jeong; Chunling Li; Chuan He; Taeok Bae
Journal:  PLoS One       Date:  2010-12-29       Impact factor: 3.240

3.  Phevalin (aureusimine B) production by Staphylococcus aureus biofilm and impacts on human keratinocyte gene expression.

Authors:  Patrick R Secor; Laura K Jennings; Garth A James; Kelly R Kirker; Elinor Delancey Pulcini; Kate McInnerney; Robin Gerlach; Tom Livinghouse; Jonathan K Hilmer; Brian Bothner; Philip Fleckman; John E Olerud; Philip S Stewart
Journal:  PLoS One       Date:  2012-07-13       Impact factor: 3.240

4.  Comparative studies on similarities and differences of cyclodipeptide oxidases for installation of C-C double bonds at the diketopiperazine ring.

Authors:  Lena Mikulski; Johanna Schäfer; Kirsten Brockmeyer; Rixa Kraut; Shu-Ming Li
Journal:  Appl Microbiol Biotechnol       Date:  2020-01-27       Impact factor: 4.813

Review 5.  Cyclic Dipeptides: The Biological and Structural Landscape with Special Focus on the Anti-Cancer Proline-Based Scaffold.

Authors:  Joanna Bojarska; Adam Mieczkowski; Zyta M Ziora; Mariusz Skwarczynski; Istvan Toth; Ahmed O Shalash; Keykavous Parang; Shaima A El-Mowafi; Eman H M Mohammed; Sherif Elnagdy; Maha AlKhazindar; Wojciech M Wolf
Journal:  Biomolecules       Date:  2021-10-14

6.  One-pot Ugi/Aza-Michael synthesis of highly substituted 2,5-diketopiperazines with anti-proliferative properties.

Authors:  Andreas Hartung; Florian Seufert; Carsten Berges; Viktoria H Gessner; Ulrike Holzgrabe
Journal:  Molecules       Date:  2012-12-11       Impact factor: 4.411
  6 in total

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