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

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 IC50 values ranging from 1.96 µM to 10.99 µM, with moderate or...

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Bibliographic Details
Main Authors: Michael Eder de Oliveira, Gisele Cenzi, Renata Rachide Nunes, Carla Regina Andrighetti, Denia Mendes de Sousa Valadão, Cláudia dos Reis, Cláudia Maria Oliveira Simões, Ricardo José Nunes, Moacyr Comar Júnior, Alex Gutterres Taranto, Bruno Antonio Marinho Sanchez, Gustavo Henrique Ribeiro Viana, Fernando de Pilla Varotti
Format: Article
Language:English
Published: MDPI AG 2013-12-01
Series:Molecules
Subjects:
4-methoxychalcone
malaria
ADMET properties
LipE
Online Access:http://www.mdpi.com/1420-3049/18/12/15276

Internet

http://www.mdpi.com/1420-3049/18/12/15276

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