69293-74-9Relevant articles and documents
tert-Butoxy-Radical-Promoted α-Arylation of Alkylamines with Aryl Halides
Ueno, Ryota,Ikeda, Yuko,Shirakawa, Eiji
supporting information, p. 4188 - 4193 (2017/08/07)
In the presence of a tert-butoxy radical precursor, the reaction of alkylamines with aryl halides was found to give α-arylated alkylamines through homolytic aromatic substitution of the halogen atoms.
Synthesis of new 4-Aminoquinolines and evaluation of their in vitro activity against chloroquine-sensitive and chloroquine-resistant plasmodium falciparum
Rajapakse, Chandima S.K.,Lisai, Maryna,Deregnaucourt, Christiane,Sinou, Véronique,Latour, Christine,Roy, Dipankar,Schrével, Joseph,Sánchez-Delgado, Roberto A.
, (2015/12/18)
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 chloroquineresistant parasites, but toxicity issues linked to a quinone-imine metabolite limit its clinical use. In search of new compounds able to retain the antimalarial activity of amodiaquine while circumventing quinone-imine metabolite toxicity, we have synthesized five 4-Aminoquinolines that feature rings lacking hydroxyl groups in the side chain of the molecules and are thus incapable of generating toxic quinone-imines. The new compounds displayed high in vitro potency (low nanomolar IC50), markedly superior to chloroquine and comparable to amodiaquine, against chloroquine-sensitive and chloroquine-resistant strains of P. falciparum, accompanied by low toxicity to L6 rat fibroblasts and MRC5 human lung cells, and metabolic stability comparable or higher than that of amodiaquine. Computational studies indicate a unique mode of binding of compound 4 to heme through the HOMO located on a biphenyl moeity, which may partly explain the high antiplasmodial activity observed for this compound.
Carboxamide compounds and their use as calpain inhibitors
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Page/Page column 42, (2008/12/08)
The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of