Literature DB >> 14611847

Prolylisoxazoles: potent inhibitors of prolyloligopeptidase with antitrypanosomal activity.

Gunther Bal1, Pieter Van der Veken, Dimitri Antonov, Anne-Marie Lambeir, Philippe Grellier, Simon L Croft, Koen Augustyns, Achiel Haemers.   

Abstract

Prolylprolylisoxazoles and prolylprolylisoxazolines were synthesized through a 1,3-dipolar cycloaddition reaction. These compounds are potent inhibitors of human and trypanosomal prolyloligopeptidase. They were shown to inhibit Trypanosoma cruzi and Trypanosoma b. brucei in in vitro systems with ED(50)'s in the lower microM range.

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Year:  2003        PMID： 14611847     DOI： 10.1016/s0960-894x(03)00579-1

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


  7 in total

1.  Identification of novel Trypanosoma cruzi prolyl oligopeptidase inhibitors by structure-based virtual screening.

Authors:  Hugo de Almeida; Vincent Leroux; Flávia Nader Motta; Philippe Grellier; Bernard Maigret; Jaime M Santana; Izabela Marques Dourado Bastos
Journal:  J Comput Aided Mol Des       Date:  2016-10-21       Impact factor: 3.686

2.  Leishmania subtilisin is a maturase for the trypanothione reductase system and contributes to disease pathology.

Authors:  Ryan K Swenerton; Giselle M Knudsen; Mohammed Sajid; Ben L Kelly; James H McKerrow
Journal:  J Biol Chem       Date:  2010-07-30       Impact factor: 5.157

3.  Tetrazole as a Replacement of the Electrophilic Group in Characteristic Prolyl Oligopeptidase Inhibitors.

Authors:  Tommi P Kilpeläinen; Jonna K Tyni; Maija K Lahtela-Kakkonen; Tony S Eteläinen; Timo T Myöhänen; Erik A A Wallén
Journal:  ACS Med Chem Lett       Date:  2019-11-11       Impact factor: 4.345

4.  The oligopeptidase B of Leishmania regulates parasite enolase and immune evasion.

Authors:  Ryan K Swenerton; Shuyi Zhang; Mohammed Sajid; Katalin F Medzihradszky; Charles S Craik; Ben L Kelly; James H McKerrow
Journal:  J Biol Chem       Date:  2010-10-20       Impact factor: 5.157

5.  Molecular, functional and structural properties of the prolyl oligopeptidase of Trypanosoma cruzi (POP Tc80), which is required for parasite entry into mammalian cells.

Authors:  Izabela M D Bastos; Philippe Grellier; Natalia F Martins; Gloria Cadavid-Restrepo; Marian R de Souza-Ault; Koen Augustyns; Antonio R L Teixeira; Joseph Schrével; Bernard Maigret; José F da Silveira; Jaime M Santana
Journal:  Biochem J       Date:  2005-05-15       Impact factor: 3.857

Review 6.  Parasite prolyl oligopeptidases and the challenge of designing chemotherapeuticals for Chagas disease, leishmaniasis and African trypanosomiasis.

Authors:  I M D Bastos; F N Motta; P Grellier; J M Santana
Journal:  Curr Med Chem       Date:  2013       Impact factor: 4.530

7.  Prolyl Oligopeptidase From Leishmania infantum: Biochemical Characterization and Involvement in Macrophage Infection.

Authors:  Camila Lasse; Clênia S Azevedo; Carla N de Araújo; Flávia N Motta; Milene A Andrade; Amanda Pereira Rocha; Iracyara Sampaio; Sébastien Charneau; Marc Gèze; Philippe Grellier; Jaime M Santana; Izabela M D Bastos
Journal:  Front Microbiol       Date:  2020-05-28       Impact factor: 5.640
  7 in total

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