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Primaquine revisited six decades after its discovery.
Presently, aablaquine and tafenoquine the two most promising primaquine analogues are already in the final stages of clinical trials against Plasmodium vivax and P. falciparum, a new hope against malaria and other primquine-sensitive illnesses, such as Pneumocystis Pneumonia or the Chagas disease. Expand
Metabolism of primaquine by liver homogenate fractions. Evidence for monoamine oxidase and cytochrome P450 involvement in the oxidative deamination of primaquine to carboxyprimaquine.
The results are consistent with an important role for MAO in primaquine biotransformation, though clearly metabolism by P450 has a contribution role. Expand
Indoloquinolines as scaffolds for drug discovery.
An overview of the potential of indoloquinolines as scaffolds in drug discovery is presented by reviewing the in vitro and in vivo biological activities of natural and synthetic analogues, as well as the proposed mechanisms of action and structure-activity relationships. Expand
Artemisinin-dipeptidyl vinyl sulfone hybrid molecules: design, synthesis and preliminary SAR for antiplasmodial activity and falcipain-2 inhibition.
A series of artemisinin-vinyl sulfone hybrid molecules with the potential to act in the parasite food vacuole via endoperoxide activation and falcipain inhibition was synthesized and screened forExpand
Targeting COPD: advances on low‐molecular‐weight inhibitors of human neutrophil elastase
There is an urgent need for low‐molecular‐weight synthetic elastase inhibitors and the present review discusses the recent advances on this field covering acylating agents, transition‐state inhibitors, mechanism‐based inhibitors, relevant natural products, and major patent disclosures. Expand
Torins are potent antimalarials that block replenishment of Plasmodium liver stage parasitophorous vacuole membrane proteins
Significance Plasmodium parasites have two distinct intracellular growth stages inside the mammalian host—the first stage, which is clinically silent, in liver hepatocytes, and the second, whichExpand
From hybrid compounds to targeted drug delivery in antimalarial therapy.
This review presents the journey that started with simple combinations of two active moieties into one chemical entity and progressed into a delivery/targeted system based on major antimalarial classes of drugs. Expand
Dipeptide Derivatives of Primaquine as Transmission-Blocking Antimalarials: Effect of Aliphatic Side-Chain Acylation on the Gametocytocidal Activity and on the Formation of Carboxyprimaquine in Rat
The title compounds prevent the development of the sporogonic cycle of Plasmodium berghei, and the presence of a terminal amino group appears to be essential for the gametocytocidal activity. Expand
Cytotoxic bile acids, but not cytoprotective species, inhibit the ordering effect of cholesterol in model membranes at physiologically active concentrations.
It was concluded that the apoptotic activity of cytotoxic BAs could be potentially associated with changes in plasma membrane organization (e.g. modulation of lipid domains) or with an increase in mitochondrial membrane affinity for apoptotic proteins. Expand
An Overview of Drug Resistance in Protozoal Diseases
In this review, drug resistance developed by protozoan parasites Plasmodium, Leishmania, and Trypanosoma will be discussed. Expand