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Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum

Malaria journal, 2013-11, Vol.12 (1), p.424-424, Article 424

2013

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Total Synthesis and Configurational Validation of (+)-Phorbaside A

Organic letters, 2010-05, Vol.12 (9), p.2158-2161

2010

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HydraScreen: A Generalizable Structure-Based Deep Learning Approach to Drug Discovery

Journal of chemical information and modeling, 2024-08, Vol.64 (15), p.5817-5831

2024

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Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

Science translational medicine, 2017-04, Vol.9 (387)

2017

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Synthesis of the Macrocyclic Core of Leiodermatolide

Organic letters, 2011-08, Vol.13 (16), p.4398-4401

2011

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Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria

Journal of medicinal chemistry, 2018-07, Vol.61 (13), p.5692-5703

2018

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UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

Antimicrobial agents and chemotherapy, 2018-09, Vol.62 (9)

2018

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Structure–activity relationship studies of antiplasmodial aminomethylthiazoles

Bioorganic & medicinal chemistry letters, 2014-11, Vol.24 (22), p.5207-5211

2014

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Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

Journal of medicinal chemistry, 2020-11, Vol.63 (21), p.13013-13030

2020

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Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts

Journal of medicinal chemistry, 2021-02, Vol.64 (4), p.2291-2309

2021

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Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria

Antimicrobial agents and chemotherapy, 2018-12, Vol.62 (12)

2018

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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

Journal of medicinal chemistry, 2018-10, Vol.61 (20), p.9371-9385

2018

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Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2

Journal of medicinal chemistry, 2014-11, Vol.57 (21), p.8839-8848

2014

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Structure–Activity-Relationship Studies around the 2‑Amino Group and Pyridine Core of Antimalarial 3,5-Diarylaminopyridines Lead to a Novel Series of Pyrazine Analogues with Oral in Vivo Activity

Journal of medicinal chemistry, 2013-11, Vol.56 (21), p.8860-8871

2013

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Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials

Journal of antimicrobial chemotherapy, 2018-05, Vol.73 (5), p.1279-1290

2018

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Structure–Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines

Journal of medicinal chemistry, 2015-09, Vol.58 (18), p.7572-7579

2015

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2,4-Diaminothienopyrimidines as Orally Active Antimalarial Agents

Journal of medicinal chemistry, 2014-02, Vol.57 (3), p.1014-1022

2014

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

Journal of medicinal chemistry, 2018-05, Vol.61 (9), p.4213-4227

2018

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Overcoming synthetic challenges in targeting coenzyme A biosynthesis with the antimicrobial natural product CJ-15,801† †Electronic supplementary information (ESI) available: Additional experimental information and electronic copies of selected spectra. See DOI: 10.1039/c9md00312f

MedChemComm, 2019-10, Vol.10 (12), p.2118-2125

2019

Volltextzugriff (PDF)

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria"

Antimicrobial agents and chemotherapy, 2018-11, Vol.62 (11)

2018

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Overcoming synthetic challenges in targeting coenzyme A biosynthesis with the antimicrobial natural product CJ-15,801

MedChemComm, 2019-12, Vol.1 (12), p.2118-2125

2019

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Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics

Malaria journal, 2014-09, Vol.13 (S1), p.38-38, Article P38

2014

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Fast in vitro methods to determine the speed of action and the stage-specificity of anti-malarials in Plasmodium falciparum

Total Synthesis and Configurational Validation of (+)-Phorbaside A

HydraScreen: A Generalizable Structure-Based Deep Learning Approach to Drug Discovery

Antimalarial efficacy of MMV390048, an inhibitor of Plasmodium phosphatidylinositol 4-kinase

Synthesis of the Macrocyclic Core of Leiodermatolide

Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria

UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria

Structure–activity relationship studies of antiplasmodial aminomethylthiazoles

Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria

Identification of a Potential Antimalarial Drug Candidate from a Series of 2‑Aminopyrazines by Optimization of Aqueous Solubility and Potency across the Parasite Life Cycle

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

Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 2

Correction to “Identification of 2,4-Disubstituted Imidazopyridines as Hemozoin Formation Inhibitors with Fast-Killing Kinetics and In Vivo Efficacy in the Plasmodium falciparum NSG Mouse Model”

A Novel Pyrazolopyridine with in Vivo Activity in Plasmodium berghei- and Plasmodium falciparum -Infected Mouse Models from Structure–Activity Relationship Studies around the Core of Recently Identified Antimalarial Imidazopyridazines

Structure–Activity-Relationship Studies around the 2‑Amino Group and Pyridine Core of Antimalarial 3,5-Diarylaminopyridines Lead to a Novel Series of Pyrazine Analogues with Oral in Vivo Activity

Potent Plasmodium falciparum gametocytocidal compounds identified by exploring the kinase inhibitor chemical space for dual active antimalarials

Structure–Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines

2,4-Diaminothienopyrimidines as Orally Active Antimalarial Agents

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

Overcoming synthetic challenges in targeting coenzyme A biosynthesis with the antimicrobial natural product CJ-15,801† †Electronic supplementary information (ESI) available: Additional experimental information and electronic copies of selected spectra. See DOI: 10.1039/c9md00312f

Erratum for Brunschwig et al., "UCT943, a Next-Generation Plasmodium falciparum PI4K Inhibitor Preclinical Candidate for the Treatment of Malaria"

Overcoming synthetic challenges in targeting coenzyme A biosynthesis with the antimicrobial natural product CJ-15,801

Identification of Plasmodium PI4 kinase as target of MMV390048 by chemoproteomics

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