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J Enzyme Inhib Med Chem ; 28(6): 1267-73, 2013 Dec.
Article in English | MEDLINE | ID: mdl-23094691

ABSTRACT

Some novel derivatives of Bis-chalcone were synthesized and characterized by their physical and spectral data. All the synthesized compounds were subsequently screened for in vitro globin hydrolysis, ß-hematin formation, and murine Plasmodium berghei, using chloroquine as the reference drug. Most of the synthesized compounds exhibited mild to moderate susceptibilities toward the parasite in comparison with the standard. The most active antimalarial compound was 1,1-Bis-[(3',4'-N-(urenylphenyl)-3-(3″,4″,5″-trimethoxyphenyl)]-2-propen-1-one 5, with a percentage of inhibition of heme polymerization of 87.05 ± 0.77, and this compound increased the survival time after infection, reduce the parasitemia and delay the progression of malaria.


Subject(s)
Antimalarials/chemical synthesis , Antimalarials/pharmacology , Chalcones/chemical synthesis , Chalcones/pharmacology , Plasmodium berghei/drug effects , Animals , Antimalarials/chemistry , Chalcones/chemistry , Dose-Response Relationship, Drug , Heme/antagonists & inhibitors , Heme/chemical synthesis , Heme/chemistry , Male , Mice , Mice, Inbred Strains , Molecular Structure , Parasitic Sensitivity Tests , Polymerization/drug effects , Structure-Activity Relationship
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