pepstatin has been researched along with Malaria* in 3 studies
3 other study(ies) available for pepstatin and Malaria
| Article | Year |
|---|---|
Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities.
The synthesis of novel chlorovinyl sulfone-like chalcone derivatives and their antimalarial activity against cultured Plasmodium falciparum parasites, hemozoin formation, hemoglobin hydrolysis and murine malaria model are described. Compounds were prepared via Claisen-Schmidt condensation from available chloromethylphenyl sulfones with substituted aldehydes. Antiplasmodial IC(50) activity of these compounds ranged between 0.025 and 10 microM, those that blocked P. falciparum development at low micro molar concentrations were tested in a murine Plasmodium berghei model, and these compounds delayed the progression of malaria but did not eradicate infections. Much effort and attention are needed for discovery and development of new and less toxic antimalarial drugs. Topics: Animals; Antimalarials; Chalcone; Hemeproteins; Hemoglobins; Humans; Hydrolysis; Malaria; Mice; Plasmodium berghei; Plasmodium falciparum; Sulfones | 2009 |
Synthesis and evaluation of sulfonylurea derivatives as novel antimalarials.
We have synthesized a series of sulfonylureas and have tested their antimalarial activities, including inhibition of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, in vitro hemoglobin hydrolysis, hemozoin formation, and development of Plasmodium berghei in murine malaria. The most active antimalarial compound was (E)-1-[4'-(3-(2,4-difluorophenyl)acryloyl)phenyl]-3-tosylurea (22) with an IC(50) of 1.2microM against cultured P. falciparum parasites. Biological results suggest a fairly potent antimalarial activity for this derivative, but also imply that its activity may arise from an unknown mechanism. Indeed, these compounds may act against malaria parasites through multiple mechanisms. Topics: Animals; Antimalarials; Chloroquine; Dose-Response Relationship, Drug; Drug Resistance; Malaria; Male; Mice; Molecular Conformation; Plasmodium berghei; Plasmodium falciparum; Sulfonylurea Compounds | 2007 |
Synthesis and evaluation of new antimalarial phenylurenyl chalcone derivatives.
Phenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteine protease falcipain-2, in vitro globin hydrolysis, beta-hematin formation, and murine Plasmodium berghei malaria. The most active antimalarial compound was 1-[3'-N-(N'-phenylurenyl)phenyl]-3(3,4,5-trimethoxyphenyl)-2-propen-1-one 49, with an IC(50) of 1.76 microM for inhibition of P. falciparum development. Results suggest that chalcones exert their antimalarial activity via multiple mechanisms. Topics: Animals; Antimalarials; Chalcones; Cysteine Endopeptidases; Globins; Heme; Hemeproteins; Hydrolysis; Malaria; Mice; Phenylurea Compounds; Plasmodium berghei; Plasmodium falciparum; Polymers; Protease Inhibitors; Structure-Activity Relationship | 2005 |