Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: Synthesis and pharmacological evaluation

Bioorganic & Medicinal Chemistry Letters
2012.0

Abstract

The synthesis and evaluation of antiplasmodial activity of benzothiazole, benzimidazole, benzoxazole and pyridine analogues of amodiaquine is hereby reported. Benzothiazole and benzoxazole analogues with a protonatable tertiary nitrogen atom possessed excellent activity against the W2 and K1 chloroquine resistant strains of Plasmodium falciparum, with IC(50)s ranging from 7 to 22 nM.

Knowledge Graph

Similar Paper

Benzoheterocyclic amodiaquine analogues with potent antiplasmodial activity: Synthesis and pharmacological evaluation
Bioorganic & Medicinal Chemistry Letters 2012.0
Antimalarial benzoheterocyclic 4-aminoquinolines: Structure–activity relationship, in vivo evaluation, mechanistic and bioactivation studies
Bioorganic & Medicinal Chemistry 2015.0
Novel amodiaquine congeners as potent antimalarial agents
Bioorganic & Medicinal Chemistry 2008.0
Structure–activity relationship studies of antiplasmodial aminomethylthiazoles
Bioorganic & Medicinal Chemistry Letters 2014.0
Syntheses and in Vitro Antiplasmodial Activity of Aminoalkylated Chalcones and Analogues
Journal of Natural Products 2015.0
4-Aminoquinoline-chalcone/- N -acetylpyrazoline conjugates: Synthesis and antiplasmodial evaluation
European Journal of Medicinal Chemistry 2017.0
Synthesis and antimalarial activity of new heterocyclic hybrids based on chloroquine and thiazolidinone scaffolds
Bioorganic & Medicinal Chemistry 2011.0
Synthesis and antiplasmodial activity of some 1-azabenzanthrone derivatives
Bioorganic & Medicinal Chemistry Letters 2013.0
Mimicking the Intramolecular Hydrogen Bond: Synthesis, Biological Evaluation, and Molecular Modeling of Benzoxazines and Quinazolines as Potential Antimalarial Agents
Journal of Medicinal Chemistry 2012.0
4-Aminoquinoline derived antimalarials: Synthesis, antiplasmodial activity and heme polymerization inhibition studies
European Journal of Medicinal Chemistry 2010.0