Literature DB >> 33361300

Tetrahydrophthalazinone Inhibitor of Phosphodiesterase with In Vitro Activity against Intracellular Trypanosomatids.

Julianna Siciliano de Araújo1, Raiza Brandão Peres1, Patrícia Bernardino da Silva1, Marcos Meuser Batista1, Geert Jan Sterk2, Louis Maes3, Guy Caljon3, Rob Leurs2, Harry P de Koning4, Titilola D Kalejaiye4, Maria de Nazaré Correia Soeiro5.   

Abstract

The phosphodiesterase inhibitor tetrahydrophthalazinone NPD-008 was explored by phenotypic in vitro screening, target validation, and ultrastructural approaches against Trypanosoma cruzi NPD-008 displayed activity against different forms and strains of T. cruzi (50% effective concentration [EC50], 6.6 to 39.5 μM). NPD-008 increased cAMP levels of T. cruzi and its combination with benznidazole gave synergistic interaction. It was also moderately active against intracellular amastigotes of Leishmania amazonensis and Leishmania infantum, confirming a potential activity profile as an antitrypanosomatid drug candidate.
Copyright © 2021 American Society for Microbiology.

Entities:  

Keywords:  L. amazonensis; L. infantum; T. cruzi; cAMP; in vitro activity; phosphodiesterase inhibitor

Mesh：

Substances：

Year:  2021        PMID： 33361300      PMCID： PMC8092546          DOI： 10.1128/AAC.00960-20

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  20 in total

1.  Synergy, antagonism, and what the chequerboard puts between them.

Authors:  F C Odds
Journal:  J Antimicrob Chemother       Date:  2003-06-12       Impact factor: 5.790

2.  Drugs and vaccines in the 21st century for neglected diseases.

Authors:  Leonardo L G Ferreira; Adriano D Andricopulo
Journal:  Lancet Infect Dis       Date:  2019-01-30       Impact factor: 25.071

3.  Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals.

Authors:  Johan Veerman; Toine van den Bergh; Kristina M Orrling; Chimed Jansen; Paul Cos; Louis Maes; Eric Chatelain; Jean-Robert Ioset; Ewald E Edink; Hermann Tenor; Thomas Seebeck; Iwan de Esch; Rob Leurs; Geert Jan Sterk
Journal:  Bioorg Med Chem       Date:  2016-02-26       Impact factor: 3.641

Review 4.  Trypanosoma cruzi genetic diversity: Something new for something known about Chagas disease manifestations, serodiagnosis and drug sensitivity.

Authors:  Bianca Zingales
Journal:  Acta Trop       Date:  2017-09-21       Impact factor: 3.112

5.  In vitro maintenance of Leishmania amastigotes directly from lesions: advantages and limitations.

Authors:  V H Hodgkinson; L Soong
Journal:  J Parasitol       Date:  1997-10       Impact factor: 1.276

6.  Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors.

Authors:  Erik de Heuvel; Abhimanyu K Singh; Ewald Edink; Tiffany van der Meer; Melanie van der Woude; Payman Sadek; Mikkel P Krell-Jørgensen; Toine van den Bergh; Johan Veerman; Guy Caljon; Titilola D Kalejaiye; Maikel Wijtmans; Louis Maes; Harry P de Koning; Geert Jan Sterk; Marco Siderius; Iwan J P de Esch; David G Brown; Rob Leurs
Journal:  Bioorg Med Chem       Date:  2019-06-18       Impact factor: 3.641

7.  Defining the role of a FYVE domain in the localization and activity of a cAMP phosphodiesterase implicated in osmoregulation in Trypanosoma cruzi.

Authors:  Alejandra C Schoijet; Kildare Miranda; Lia Carolina Soares Medeiros; Wanderley de Souza; Mirtha M Flawiá; Héctor N Torres; Omar P Pignataro; Roberto Docampo; Guillermo D Alonso
Journal:  Mol Microbiol       Date:  2010-10-28       Impact factor: 3.501

8.  Alkynamide phthalazinones as a new class of TbrPDEB1 inhibitors (Part 2).

Authors:  Erik de Heuvel; Abhimanyu K Singh; Pierre Boronat; Albert J Kooistra; Tiffany van der Meer; Payman Sadek; Antoni R Blaazer; Nathan C Shaner; Daphne S Bindels; Guy Caljon; Louis Maes; Geert Jan Sterk; Marco Siderius; Michael Oberholzer; Iwan J P de Esch; David G Brown; Rob Leurs
Journal:  Bioorg Med Chem       Date:  2019-07-05       Impact factor: 3.641

9.  Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi.

Authors:  Julianna Siciliano De Araújo; Patrícia Bernardino da Silva; Marcos Meuser Batista; Raiza Brandão Peres; Camila Cardoso-Santos; Titilola D Kalejaiye; Jane C Munday; Erik De Heuvel; Geert Jan Sterk; Koen Augustyns; Irene G Salado; An Matheeussen; Iwan De Esch; Harry P De Koning; Rob Leurs; Louis Maes; Maria de Nazaré Correia Soeiro
Journal:  J Antimicrob Chemother       Date:  2020-04-01       Impact factor: 5.790

10.  Targeting a Subpocket in Trypanosoma brucei Phosphodiesterase B1 (TbrPDEB1) Enables the Structure-Based Discovery of Selective Inhibitors with Trypanocidal Activity.

Authors:  Antoni R Blaazer; Abhimanyu K Singh; Erik de Heuvel; Ewald Edink; Kristina M Orrling; Johan J N Veerman; Toine van den Bergh; Chimed Jansen; Erin Balasubramaniam; Wouter J Mooij; Hans Custers; Maarten Sijm; Daniel N A Tagoe; Titilola D Kalejaiye; Jane C Munday; Hermann Tenor; An Matheeussen; Maikel Wijtmans; Marco Siderius; Chris de Graaf; Louis Maes; Harry P de Koning; David S Bailey; Geert Jan Sterk; Iwan J P de Esch; David G Brown; Rob Leurs
Journal:  J Med Chem       Date:  2018-05-01       Impact factor: 7.446
View more
  1 in total

1.  Perspectives for a new drug candidate for Chagas disease therapy.

Authors:  Maria de Nazaré Correia Soeiro
Journal:  Mem Inst Oswaldo Cruz       Date:  2022-03-14       Impact factor: 2.743
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.