Murugesan, Dinakaran; Kaiser, Marcel; White, Karen L.; Norval, Suzanne; Riley, Jennifer; Wyatt, Paul G.; Charman, Susan A.; Read, Kevin D.; Yeates, Clive; Gilbert, Ian H. published an article in 2013, the title of the article was Structure-Activity Relationship Studies of Pyrrolone Antimalarial Agents.Related Products of 386704-04-7 And the article contains the following content:
Previously reported pyrrolones, such as TDR32570 (I), exhibited potential as antimalarial agents; however, while these compounds have potent antimalarial activity, they suffer from poor aqueous solubility and metabolic instability. Here, further structure-activity relationship studies are described that aimed to solve the developability issues associated with this series of compounds In particular, further modifications to the lead pyrrolone, involving replacement of a Ph ring with a piperidine and removal of a potentially metabolically labile ester by a scaffold hop, gave rise to derivatives with improved in vitro antimalarial activities against Plasmodium falciparum K1, a chloroquine- and pyrimethamine-resistant parasite strain, with some derivatives exhibiting good selectivity for parasite over mammalian (L6) cells. Three representative compounds were selected for evaluation in a rodent model of malaria infection, and the best compound showed improved ability to decrease parasitemia and a slight increase in survival. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Related Products of 386704-04-7
The Article related to pyrrolone piperidine containing preparation antimalarial structure activity relationship, plasmodium falciparum, antiprotozoal agents, malaria, pyrrolones, structure-activity relationships and other aspects.Related Products of 386704-04-7
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