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Antimalarial Activity of 4-Metoxychalcones: Docking Studies as Falcipain/Plasmepsin Inhibitors, ADMET and Lipophilic Efficiency Analysis to Identify a Putative Oral Lead Candidate

Herein, we report the antimalarial activity of nine 4-methoxychalcone derivatives 1a–i and an initial analysis of their ADMET properties. All compounds showed potent activity against the P. falciparum chloroquine-resistant clone W2, with IC(50) values ranging from 1.96 µM to 10.99 µM, with moderate...

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Detalles Bibliográficos
Autores principales: de Oliveira, Michael Eder, Cenzi, Gisele, Nunes, Renata Rachide, Andrighetti, Carla Regina, de Sousa Valadão, Denia Mendes, dos Reis, Cláudia, Simões, Cláudia Maria Oliveira, Nunes, Ricardo José, Júnior, Moacyr Comar, Taranto, Alex Gutterres, Sanchez, Bruno Antonio Marinho, Viana, Gustavo Henrique Ribeiro, de Pilla Varotti, Fernando
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2013
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6269736/
https://www.ncbi.nlm.nih.gov/pubmed/24335577
http://dx.doi.org/10.3390/molecules181215276