Literature DB >> 20561792

Development of tryptase inhibitors derived from thalidomide.

Masashi Tetsuhashi1, Minoru Ishikawa, Mariko Hashimoto, Yuichi Hashimoto, Hiroshi Aoyama.   

Abstract

A novel series of tryptase inhibitors with a N-phenylphthalimide skeleton structurally derived from thalidomide (1) has been developed. Structure-activity relationship studies led to a potent and selective tryptase inhibitor, 2-(4-cyanophenyl)isoindole-1,3-dione-5-yl 3-(2-aminopyridin-5-yl)propanoate (7), with the IC50 value of 78 nM. Copyright (c) 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20561792     DOI: 10.1016/j.bmc.2010.05.037

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


  3 in total

1.  Triplex-Forming Peptide Nucleic Acids with Extended Backbones.

Authors:  Vipin Kumar; Nikita Brodyagin; Eriks Rozners
Journal:  Chembiochem       Date:  2020-08-31       Impact factor: 3.164

2.  Study on the synthesis of novel 5-substituted 2-[2-(pyridyl)ethenyl]-1,3,4-oxadiazoles and their acid-base interactions.

Authors:  Agnieszka Kudelko; Karolina Jasiak; Krzysztof Ejsmont
Journal:  Monatsh Chem       Date:  2014-12-20       Impact factor: 1.451

3.  Discovery of potent inhibitors of human β-tryptase from pre-equilibrated dynamic combinatorial libraries.

Authors:  Qian-Qian Jiang; Wilhelm Sicking; Martin Ehlers; Carsten Schmuck
Journal:  Chem Sci       Date:  2014-12-08       Impact factor: 9.825

  3 in total

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