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 |
|---|---|
| Přispěvatelé: | AIMMS, Medicinal chemistry |
| Jazyk: | angličtina |
| Rok vydání: | 2021 |
| Předmět: |
L. amazonensis
Trypanosoma cruzi Leishmania mexicana Antiprotozoal Agents Microbiology 03 medical and health sciences SDG 3 - Good Health and Well-being parasitic diseases medicine Humans In vitro activity Experimental Therapeutics Chagas Disease Pharmacology (medical) Phosphodiesterase inhibitor Amastigote Biology 030304 developmental biology Pharmacology 0303 health sciences biology Phosphoric Diester Hydrolases 030306 microbiology Chemistry Pharmacology. Therapy Phosphodiesterase biology.organism_classification In vitro L. infantum T. cruzi 3. Good health Infectious Diseases Benznidazole Human medicine Leishmania infantum CAMP Intracellular medicine.drug |
| Zdroj: | 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 |
| ISSN: | 1098-6596 0066-4804 |
| DOI: | 10.1128/AAC.00960-20 |
| Popis: | 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 [EC 50 ], 6.6 to 39.5 μM). Increased cAMP levels of T. cruzi and its combination with benznidazole gave synergistic interaction. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|