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-(3â³,4â³,5â³-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 RelationshipABSTRACT
A series of new benzenesulfonamides, most of which are chiral, incorporating 1, 3, 4-oxadiazole and amino acid moieties have been synthesized. Some of these compounds were screened for antimalarial activity and also evaluated for their ability to inhibit hem polymerization. The electrophoretic analysis indicated that one compound was effective in inhibiting the degradation of hemoglobin. The synthesized compounds were tested in mice infected with Plasmodium berghei. These derivatives have the potential for the development of novel antimalarial lead compounds.
