Background & Aim: Antiplasmodial activity of leaf extract of Breynia nivosa was evaluated to ascertain the folkloric claim of its antimalarial activity. Experimental: The crude leaf extract (75 – 225 mg/kg), of Breynia nivosa was investigated for antiplasmodial activity against chloroquine sensitive Plasmodium berghei infections in mice. The antiplasmodial activity d...

Pafuramidine is a novel orally active antimalarial. To identify a combination partner, we measured the in vitro antimalarial activities of the active metabolite, DB75, with amodiaquine, artemisinin, atovaquone, azithromycin, chloroquine, clindamycin, mefloquine, piperaquine, pyronaridine, tafenoquine, and tetracycline. None of the drugs tested demonstrated antagonistic or synergistic activity i...

Unsymmetrical dispiro- and spirotetraoxanes have been designed and synthesized via acid-catalyzed cyclocondensation of bis(hydroperoxides) with ketones. Incorporation of water-soluble and polar functionalities, via reductive amination and amide bond formation, produces several analogues with low nanomolar in vitro antimalarial activity. Several analogues display an unprecedented level of oral a...

Artemisinin and its derivatives are endoperoxide-containing compounds which represent a promising new class of antimalarial drugs. In the presence of intraparasitic iron, these drugs are converted into free radicals and other electrophilic intermediates which then alkylate specific malaria target proteins. Combinations of available derivatives and other antimalarial agents show promise both as ...

calotropis procera is a small, erect plant, which is used in several traditional medicines to treat many diseases. it is a native of most of the asian and african countries. all plant parts exude thick white milky juice (latex) on cut or break. this shrub has been known to possess analgesic, antitumor, antihelmintic, antioxidant, hepatoprotective, antidiarrhoeal, anticonvulsant, antimicrobial, ...

The in vivo alkylation of heme by the antimalarial trioxaquine DU1301 afforded covalent heme-drug adducts that were detected in the spleens of Plasmodium sp.-infected mice. This result indicates that the alkylation capacities of trioxaquines in mammals infected with Plasmodium strains are similar to that of artemisinin, a natural antimalarial trioxane-containing drug.

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 ...

The MIC of an antimalarial drug for a particular infection is the drug level associated with a net parasite multiplication rate of one per asexual cycle. To ensure the cure of malaria, the MIC must be exceeded until all parasites have been eliminated. The development of highly sensitive and accurate PCR quantitation of low-density malaria parasitemia enables the prospective pharmacokinetic-phar...

Malaria is a mosquito-borne lifethreatening disease. Though it is treatable but due to emerging resistance against well-known drugs like 8aminoquinolines and artemisinin analogs, it is urgent need to develop novel drugs for the treatment of malaria. In order to develop a new drug, imidazolopiperazine derivatives have been shown antimalarial efficacy against wild-type as well as drug resistant m...

BACKGROUND The problem of resistance of malarial parasites to available antimalarial drugs makes the development of new drugs imperative, with natural plant products providing an alternative source for discovering new drugs. AIM To evaluate the antimalarial activity of eluted fractions of Acacia nilotica root extract and determine the phytochemicals responsible for its antimalarial activity. ...