Tetrahydrophthalazinone inhibitor of phosphodiesterase with in vitro activity against intracellular trypanosomatids

Autor: Guy Caljon, Louis Maes, Geert Jan Sterk, Maria de Nazaré Correia Soeiro, Raiza Brandão Peres, Titilola D. Kalejaiye, Julianna Siciliano de Araújo, Rob Leurs, Patrícia Bernardino da Silva, Marcos Meuser Batista, Harry P. de Koning

Publikováno v: De Araújo, J S, Peres, R B, Da Silva, P B, Batista, M M, Sterk, G J, Maes, L, Caljon, G, Leurs, R, De Koning, H P, Kalejaiye, T D & De Nazaré Correia Soeiro, M 2021, ' Tetrahydrophthalazinone inhibitor of phosphodiesterase with in vitro activity against intracellular trypanosomatids ', Antimicrobial agents and chemotherapy, vol. 65, no. 3, e00960-20, pp. 1-5 . https://doi.org/10.1128/AAC.00960-20
Antimicrob Agents Chemother
Antimicrobial agents and chemotherapy, 65(3):e00960-20, 1-5. American Society for Microbiology
Antimicrobial agents and chemotherapy

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 strain

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::32c53fb735539c1613c3b6501c2337e4
https://doi.org/10.1128/AAC.00960-20

Efficacy of Novel Pyrazolone Phosphodiesterase Inhibitors in Experimental Mouse Models of Trypanosoma cruzi

Autor: Geert Jan Sterk, Titilola D. Kalejaiye, Cristiane França da Silva, Julianna Siciliano de Araújo, Maarten Sijm, Rob Leurs, Ludmila Ferreira de Almeida Fiuza, Harry P. de Koning, Cristina Fonseca-Berzal, Denise da Gama Jaen Batista, Louis Maes, Maria de Nazaré Correia Soeiro, A. S. G. Nefertiti, Marcos Meuser Batista, Patrícia Bernardino da Silva

Publikováno v: Antimicrobial agents and chemotherapy, 64(9):e00414-20, 1-11. American Society for Microbiology
Antimicrobial agents and chemotherapy
de Araújo, J S, França da Silva, C, Batista, D D G J, Nefertiti, A, Fiuza, L F D A, Fonseca-Berzal, C R, Bernardino da Silva, P, Batista, M M, Sijm, M, Kalejaiye, T D, de Koning, H P, Maes, L, Sterk, G J, Leurs, R & Soeiro, M D N C 2020, ' Efficacy of Novel Pyrazolone Phosphodiesterase Inhibitors in Experimental Mouse Models of Trypanosoma cruzi ', Antimicrobial agents and chemotherapy, vol. 64, no. 9, e00414-20, pp. 1-11 . https://doi.org/10.1128/AAC.00414-20
Antimicrob Agents Chemother

Pyrazolones are heterocyclic compounds with interesting biological properties. Some derivatives inhibit phosphodiesterases (PDEs) and thereby increase the cellular concentration of cyclic AMP (cAMP), which plays a vital role in the control of metabol

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4cfe21cadb9de1ab732be994c539a37c
https://research.vu.nl/en/publications/60532e52-ce8d-4c5f-8df6-e8d9f01083b2

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

Autor: Jane C. Munday, An Matheeussen, Camila Cardoso-Santos, Titilola D. Kalejaiye, Marcos Meuser Batista, Rob Leurs, Iwan J. P. de Esch, Harry P. de Koning, Maria de Nazaré Correia Soeiro, Patrícia Bernardino da Silva, Irene G. Salado, Louis Maes, Erik de Heuvel, Raiza Brandão Peres, Geert Jan Sterk, Koen Augustyns, Julianna Siciliano de Araújo

Publikováno v: Journal of antimicrobial chemotherapy, 75(4), 958-967. Oxford University Press
The journal of antimicrobial chemotherapy
De Araújo, J S, da Silva, P B, Batista, M M, Peres, R B, Cardoso-Santos, C, Kalejaiye, T D, Munday, J C, De Heuvel, E, Sterk, G J, Augustyns, K, Salado, I G, Matheeussen, A, De Esch, I, De Koning, H P, Leurs, R, Maes, L & Soeiro, M D N C 2020, ' Evaluation of phthalazinone phosphodiesterase inhibitors with improved activity and selectivity against Trypanosoma cruzi ', Journal of antimicrobial chemotherapy, vol. 75, no. 4, pp. 958-967 . https://doi.org/10.1093/jac/dkz516

Background Chagas’ disease, caused by the protozoan parasite Trypanosoma cruzi, needs urgent alternative therapeutic options as the treatments currently available display severe limitations, mainly related to efficacy and toxicity. Objectives As ph

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a8ddcd06a37b70f7392d21298a13bf2a
https://pubmed.ncbi.nlm.nih.gov/31860098

Phenotypic evaluation and in silico ADMET properties of novel arylimidamides in acute mouse models of

Autor: Cristiane França, da Silva, Denise da Gama Jaén, Batista, Julianna Siciliano, de Araújo, Edézio Ferreira, Cunha-Junior, Chad E, Stephens, Moloy, Banerjee, Abdelbasset A, Farahat, Senol, Akay, Mary K, Fisher, David W, Boykin, Maria de Nazaré Correia, Soeiro

Publikováno v: Drug Design, Development and Therapy

Arylimidamides (AIAs), previously termed as reversed amidines, present a broad spectrum of activity against intracellular microorganisms. In the present study, three novel AIAs were evaluated in a mouse model of Trypanosoma cruzi infection, which is

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::9217e09077be2be70c676f8097b1a592
https://pubmed.ncbi.nlm.nih.gov/28435221

In Vitro and In Vivo Trypanosomicidal Action of Novel Arylimidamides against Trypanosoma cruzi

Autor: Donald A. Patrick, R R Tidwell, Maria de Nazaré Correia Soeiro, Otacilio C. Moreira, C. F. Da Silva, P. B. Da Silva, Kelly Cristina Demarque, Svetlana M. Bakunova, Constança Britto, Stanislav A. Bakunov, T. O. Fulco, Julianna Siciliano de Araújo, F. H. Guedes-da-Silva, Gilkethyla Mexlayne de Oliveira, D. G. J. Batista, M. B. Meuser

Arylimidamides (AIAs) have been shown to have considerable biological activity against intracellular pathogens, including Trypanosoma cruzi , which causes Chagas disease. In the present study, the activities of 12 novel bis-AIAs and 2 mono-AIAs again

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9931d7933fdd07aea27acf8c429ef9b4
https://europepmc.org/articles/PMC4808220/