The emergence and spread of drug resistant malaria represents a considerable challenge to controlling malaria. To date, malaria control has relied heavily on a comparatively small number of chemically related drugs, belonging to either the quinoline or the antifolate groups. Only recently have the artemisinin derivatives been used but mostly in south east Asia. Experience has shown that resista...

Between 1998 and 2001, Kenya, Uganda, Tanzania, Zanzibar, Rwanda and Burundi changed antimalarial drug policy, in the face of widespread chloroquine resistance. The new first-line treatment is either sulphadoxine–pyrimethamine (SP) monotherapy, or a combination of SP with either chloroquine or amodiaquine. Two national malaria control programmes, Burundi and Zanzibar, have decided upon amodiaqu...

We synthesized C-10 substituted triazolyl artemisinins by the Huisgen cycloaddition reaction between dihydroartemisinins (2) and variously substituted 1, 2, 3-triazoles (8a-8h). The antimalarial activities of 32 novel artemisinin derivatives were screened against a chloroquine-resistant parasite. Among them, triazolyl artemisinins with electron-withdrawing groups showed stronger antimalarial ac...

The evaluation of new antimalarial agents using older methods of monitoring sensitivity to antimalarial drugs are laborious and poorly suited to discriminate stage-specific activity. We used flow cytometry to study the effect of established antimalarial compounds, cysteine protease inhibitors, and a quinolone against asexual stages of Plasmodium falciparum. Cultured P. falciparum parasites were...

Five primaquine (PQ) analogues have been isolated by peroxydisulfate oxidation and were tested for antimalarial activity against Plasmodium yoelli infected mice. To develop them as promising antimalarial agents in-silico druglikeness studies were carried out. The analogue 6-Methoxy-5,8-di-(4-amino-1-methylbutyl-amino)-quinoline [P1] was found to be promising antimalarial agent as it was found n...

Malaria is one of the top health problems in Yemen. This study was done to evaluate the availabilit and prescribing of antimalarial drugs in Al-Mukalla city, based on the treatment guidelines of the National Malari Control Programme (NMCP). Chloroquine, quinine and sulfadoxine/pyrimethamine were the most availabl and prescribed antimalarial drugs in all 60 pharmacies (government and private) in...

A set of benzophenone derivatives was evaluated for the antimalarial activity against Plasmodium berghei in mice and the mean survival time of mice for all the compounds was determined. The QSAR analysis was carried out for the fourteen benzophenone derivatives using different physicochemical descriptors. The multiple linear regression analysis was used to correlate the physicochemical descript...

Background: Malaria remains the world’s most devastating human parasitic infection. Our goal was to assess the capacity of increasing concentrations of five antimalarial drugs (FansidarTM, HalfanTM, Quinine, CoartemTM and Chloroquine phosphate) to elicit the generation of methemoglobin in three human erythrocyte genotypes (Hb AA, Hb AS and Hb SS). Materials and Methods: Spectrophotometric metho...

Quinazolinedione is one of the most notable pharmacophores in drug discovery due to its broad spectrum biological activities including antimalarial, anticancer, anti-inflammatory, and others. TCMDC-125133, whose structure features a quinazolinedione core, exhibits promising antimalarial activity low toxicity as described GlaxoSmithKline (GSK) report. Herein, concise four-step synthesis towards ...

Despite considerable efforts, malaria is still one of the most devastating infectious diseases in the tropics. The rapid spread of antimalarial drug resistance currently compounds this grim picture. In this paper, we review the history of antimalarial drug resistance and the methods for monitoring it and assess the current magnitude and burden of parasite resistance to two commonly used drugs: ...