Abstract: Malaria is a potentially fatal parasitic disease brought on by five Plasmodium species, including falciparum, vivax, ovale, malariae, and knowlesi. The fast emergence of P. falciparum resistance to currently available treatments has increased health concerns in developing countries. growth emphasizes the need for novel, secure, cost-effective antimalarial drug that can treat malaria r...

A transition-metal-free and base-promoted one-pot reaction of ynones with 2-aminobenzonitriles is described. The was initiated through sequential aza-Michael addition/intramolecular annulation to afford various multisubstituted 4-aminoquinolines 4-amino-1,8-naphthyridines in good excellent yields. Operational simplicity, high atom-economy broad substrate scope makes this protocol more attractiv...

The antimicrobial activities of chloroquine (CQ) and several 4-aminoquinoline drugs were tested against Penicillium marneffei, an opportunistic fungus that invades and grows inside macrophages and causes disseminated infection in AIDS patients. Human THP1 and mouse J774 macrophages were infected in vitro with P. marneffei conidia and treated with different doses of drugs for 24 to 48 h followed...

Imidazolidin-4-one derivatives of primaquine were synthesized as potential double prodrugs of the parent drug. The title compounds inhibit the development of the sporogonic cycle of Plasmodium berghei, affecting the appearance of oocysts in the midguts of the mosquitoes. The imidazolidin-4-ones are very stable, both in human plasma and in pH 7.4 buffer, indicating that they are active per se. T...

The in vitro activities of pyronaridine, alone and in combination with established antimalarial drugs, were assessed by isotopic microtest. Pyronaridine was highly active against all Cameroonian isolates. A positive correlation was observed between the response to pyronaridine and that to chloroquine. Drug combination studies showed synergy between pyronaridine and primaquine, additive effects ...

The efficacy of chloroquine, once the drug of choice in the fight against Plasmodium falciparum, is now severely limited due to widespread resistance. Amodiaquine is one of the most potent antimalarial 4-aminoquinolines known and remains effective against chloroquine-resistant parasites, but toxicity issues linked to a quinone-imine metabolite limit its clinical use. In search of new compounds ...

The emergence and rapid spread of chloroquine resistant strains of Plasmodium falciparum has dramatically reduced the chemotherapeutic options. Towards this goal, the quantitative structure-activity relationship analysis of some synthesized 7-substituted 4aminoquinolines were performed for their antiplasmodial activity against chloroquine-resistant parasites to find out the structural features ...

For several decades, the 4-aminoquinolines chloroquine (CQ) and amodiaquine (AQ) were considered the most important drugs for the control and eradication of malaria. The success of this class has been based on excellent clinical efficacy, limited host toxicity, ease of use and simple, cost-effective synthesis. Importantly, chloroquine therapy is affordable enough for use in the developing world...

A series of primaquine-derived imidazolidin-4-ones were screened for their in vitro activity against Pneumocystis carinii and Plasmodium falciparum W2 strain. Most compounds were active against P. carinii above 10 microg/mL and displayed slight to marked activity. The imidazolidin-4-ones most active against P. carinii were also those most active antiplasmodial agents, in the muM range. One of t...

We provide two simple low-cost and low-tech procedures to measure with good precision and accuracy the binding and internalization into human erythrocytes of chloroquine and other aminoquinolines. The methods are based on the high fluorescence of the quinoline ring and are complementary. Method A evaluates residual drugs in the supernatants of treated erythrocytes, whereas method B quantifies t...