New ferrocenic pyrrolo[1,2-a]quinoxaline derivatives: Synthesis, and in vitro antimalarial activity – Part II

Models, Molecular Dose-Response Relationship, Drug Molecular Structure Metallocenes [SDV]Life Sciences [q-bio] Plasmodium falciparum Drug Evaluation, Preclinical Stereoisomerism Crystallography, X-Ray 01 natural sciences Cell Line 3. Good health 0104 chemical sciences Antimalarials Structure-Activity Relationship [SDV.MP]Life Sciences [q-bio]/Microbiology and Parasitology Parasitic Sensitivity Tests Quinoxalines [CHIM]Chemical Sciences Humans Pyrroles Ferrous Compounds Cell Proliferation
DOI: 10.1016/j.ejmech.2011.03.014 Publication Date: 2011-03-16T08:20:17Z
ABSTRACT
Following our search for antimalarial compounds, novel series of ferrocenyl-substituted pyrrolo[1,2-a]quinoxalines 1-2 were synthesized from ferrocene-carboxaldehyde and tested for their in vitro activity upon the erythrocytic development of Plasmodium falciparum strains with different chloroquine-resistance status. The ferrocenic pyrrolo[1,2-a]quinoxalines 1-2 were prepared in 6 or 9 steps through a Barton-Zard reaction. Promising pharmacological results against FcB1, K1 and F32 strains were obtained with ferrocenyl pyrrolo[1,2-a]quinoxalines 1j-l linked by a bis-(3-aminopropyl)piperazine linker substituted by a nitrobenzyl moiety.
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