Pyridazino-pyrrolo-quinoxalinium salts as highly potent and selective leishmanicidal agents targeting trypanothione reductase

ABSTRACT: Fifteen pyridazino-pyrrolo-quinoxalinium salts were synthesized and tested for their antiprotozoal activity against Leishmania infantum amastigotes. Eleven of them turned out to be leishmanicidal, with EC50 values in the nanomolar range, and displayed low toxicity against the human THP-1 c...

Full description

Autores:

Toro Londoño, Miguel Ángel
de Lucio, Héctor
García Marín, Javier
Sánchez Alonso, Patricia
García-Soriano, Juan Carlos
Vaquero, Juan J.
Gago, Federico
Alajarín, Ramón
Jiménez Ruiz, Antonio

Tipo de recurso:

Article of investigation

Fecha de publicación:

2022

Institución:

Universidad de Antioquia

Repositorio:

Repositorio UdeA

Idioma:

eng

OAI Identifier:

oai:bibliotecadigital.udea.edu.co:10495/44131

Acceso en línea:

https://hdl.handle.net/10495/44131

Palabra clave:

Antiprotozoarios
Antiprotozoal Agents
Relación Dosis-Respuesta a Droga
Dose-Response Relationship, Drug
Inhibidores Enzimáticos
Enzyme Inhibitors
Leishmania infantum
Estructura Molecular
Molecular Structure
NADH NADPH Oxidorreductasas
NADH, NADPH Oxidoreductases
Pruebas de Sensibilidad Parasitaria
Parasitic Sensitivity Tests
Piridazinas
Pyridazines
Pirroles
Pyrroles
Quinoxalinas
Quinoxalines
Sales (Química)
Salts
Relación Estructura-Actividad
Structure-Activity Relationship
Células THP-1
THP-1 Cells
https://id.nlm.nih.gov/mesh/D000981
https://id.nlm.nih.gov/mesh/D004305
https://id.nlm.nih.gov/mesh/D004791
https://id.nlm.nih.gov/mesh/D018314
https://id.nlm.nih.gov/mesh/D015394
https://id.nlm.nih.gov/mesh/D009247
https://id.nlm.nih.gov/mesh/D021261
https://id.nlm.nih.gov/mesh/D011724
https://id.nlm.nih.gov/mesh/D011758
https://id.nlm.nih.gov/mesh/D011810
https://id.nlm.nih.gov/mesh/D012492
https://id.nlm.nih.gov/mesh/D013329
https://id.nlm.nih.gov/mesh/D000074084

Rights

openAccess

License

https://creativecommons.org/licenses/by-nc-nd/2.5/co/