Bokosi, Fostino R. B.; Beteck, Richard M.; Mbaba, Mziyanda; Mtshare, Thanduxolo E.; Laming, Dustin; Hoppe, Heinrich C.; Khanye, Setshaba D. published the artcile< Design, synthesis and biological evaluation of mono- and bisquinoline methanamine derivatives as potential antiplasmodial agents>, Product Details of C6H8N2, the main research area is quinoline methanamine preparation antimalarial; Antiplasmodial; Chloroquine-sensitive; Plasmodium falciparum; Quinoline.
Several classes of antimalarial drugs are currently available, although issues of toxicity and the emergence of drug resistant malaria parasites have reduced their overall therapeutic efficiency. Quinoline based antiplasmodial drugs have unequivocally been long-established and continue to inspire the design of new antimalarial agents. Herein, a series of mono- and bisquinoline methanamine derivatives were synthesized through sequential steps; Vilsmeier-Haack, reductive amination, and nucleophilic substitution, and obtained in low to excellent yields. The resulting compounds were investigated for in vitro antiplasmodial activity against the 3D7 chloroquine-sensitive strain of Plasmodium falciparum, and compounds I and II emerged as the most promising with IC50 values of 0.23 and 0.93μM, resp. The most promising compounds were also evaluated in silico by mol. docking protocols for binding affinity to the {0 0 1} fast-growing face of a hemozoin crystal model.
Bioorganic & Medicinal Chemistry Letters published new progress about Amines Role: PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 3731-53-1 belongs to class pyridine-derivatives, and the molecular formula is C6H8N2, Product Details of C6H8N2.