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 activities of total extracts and lupane triterpenes, isolated from the stem bark of Acacia mellifera, were evaluated against Plasmodium berghei strain ANKA in a female Swiss mouse model. Five isolated compounds and the crude extracts were evaluated for antimalarial activity and Quinine hydrochloride was used as a positive control. Only betulin and the methanolic extract produced considerabl...

The abietane-type diterpenoid (+)-ferruginol, a bioactive compound isolated from New Zealand's Miro tree (Podocarpus ferruginea), displays relevant pharmacological properties, including antimicrobial, cardioprotective, anti-oxidative, anti-plasmodial, leishmanicidal, anti-ulcerogenic, anti-inflammatory and anticancer. Herein, we demonstrate that ferruginol (1) and some phthalimide containing an...

Thirty weak base 1,2,4-dispiro trioxolanes (secondary ozonides) were synthesized. Amino amide trioxolanes had the best combination of antimalarial and biopharmaceutical properties. Guanidine, aminoxy, and amino acid trioxolanes had poor antimalarial activity. Lipophilic trioxolanes were less stable metabolically than their more polar counterparts.

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...

A microemulsion preconcentrate was formulated on the basis of solubility of artemether (ARM) in the various oily phases and surfactants and phase diagrams. Various solid adsorbents were evaluated for their ability yield solid microemulsion preconcentrates (NanOsorb-ARM). NanOsorb-ARM on dilution yielded microemulsion with average globule size of 183 nm and polydispersity index of 0.498 when det...

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...

Artemisinin, a sesquiterpene with endoperoxide bond, possesses potent antimalarial activity against the ring and late stage of chloroqine-resistant Plasmodium falciparum malaria both in vitro and in vivo. The mode of antimalarial activity of artemisinin is iron-dependent. The aim of this study was to investigate the reactions of artemisinin with ferrous and ferric ions in aqueous buffer. Artemi...

Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains examined. The compounds showed moderate in vitro antimalarial two P. falciparum strains, 3D7 (CQ susceptible clone) Dd2 resistant clone). Three aminoquinolines were further examined for efficacy a mouse model using modified Thompson test. In this model, mice infected with berghei-infec...