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Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains

scientific article published on 16 October 2018

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies

artículo científico publicado en 2015

Bayesian models trained with HTS data for predicting β-haematin inhibition and in vitro antimalarial activity.

artículo científico publicado en 2014

Emerging Southeast Asian PfCRT mutations confer Plasmodium falciparum resistance to the first-line antimalarial piperaquine

artículo científico publicado en 2018

Identification and Mechanistic Evaluation of Hemozoin-Inhibiting Triarylimidazoles Active against Plasmodium falciparum

artículo científico publicado en 2017

Identification and SAR Evaluation of Hemozoin-Inhibiting Benzamides Active against Plasmodium falciparum.

artículo científico publicado en 2016

Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ null Mouse Model of Malaria.

artículo científico publicado en 2018

Identification of β-hematin inhibitors in a high-throughput screening effort reveals scaffolds with in vitro antimalarial activity.

artículo científico publicado en 2014

In vitro antimalarial activity, β-haematin inhibition and structure-activity relationships in a series of quinoline triazoles

artículo científico publicado en 2013

Inhibition of Resistance-Refractory P. falciparum Kinase PKG Delivers Prophylactic, Blood Stage, and Transmission-Blocking Antiplasmodial Activity

artículo científico publicado en 2020

N10,N11-di-alkylamine indolo[3,2-b]quinolines as hemozoin inhibitors: design, synthesis and antiplasmodial activity

artículo científico publicado en 2015

Structure and drug resistance of the Plasmodium falciparum transporter PfCRT

scientific article published on 27 November 2019

Synthesis and antimalarial testing of neocryptolepine analogues: addition of ester function in SAR study of 2,11-disubstituted indolo[2,3-b]quinolines.

artículo científico publicado en 2013

Synthesis and in vitro testing of antimalarial activity of non-natural-type neocryptolepines: structure–activity relationship study of 2,11- and 9,11-disubstituted 6-methylindolo[2,3-b]quinolines.

artículo científico publicado en 2013

Synthesis, β-haematin inhibition, and in vitro antimalarial testing of isocryptolepine analogues: SAR study of indolo[3,2-c]quinolines with various substituents at C2, C6, and N11.

artículo científico publicado en 2014