Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7

Bioorganic & Medicinal Chemistry Letters
2008.0

Abstract

A high-throughput screening campaign identified a number of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7. Further synthetic chemistry efforts enabled the preparation of a number of analogues with promising in vitro potencies. Although these compounds show likely broad spectrum inhibitory activity, they represent a useful starting point for further chemical optimisation.

Knowledge Graph

Similar Paper

Synthesis and in vitro evaluation of imidazopyridazines as novel inhibitors of the malarial kinase PfPK7
Bioorganic & Medicinal Chemistry Letters 2008.0
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 2020.0
Trisubstituted thiazoles as potent and selective inhibitors of Plasmodium falciparum protein kinase G (PfPKG)
Bioorganic & Medicinal Chemistry Letters 2018.0
Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor
European Journal of Medicinal Chemistry 2017.0
Medicinal Chemistry Optimization of Antiplasmodial Imidazopyridazine Hits from High Throughput Screening of a SoftFocus Kinase Library: Part 1
Journal of Medicinal Chemistry 2014.0
Identification of Fast-Acting 2,6-Disubstituted Imidazopyridines That Are Efficacious in the in Vivo Humanized Plasmodium falciparum NODscidIL2Rγ<sup>null</sup> Mouse Model of Malaria
Journal of Medicinal Chemistry 2018.0
Evaluation of the anti-malarial activity and cytotoxicity of 2,4-diamino-pyrimidine-based kinase inhibitors
European Journal of Medicinal Chemistry 2016.0
Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials
Bioorganic &amp; Medicinal Chemistry Letters 2010.0
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
Journal of Medicinal Chemistry 2015.0
Development of new highly potent imidazo[1,2-b]pyridazines targeting Toxoplasma gondii calcium-dependent protein kinase 1
European Journal of Medicinal Chemistry 2015.0