Catalyst controlled remote CH activation of 8-aminoquinolines with NFSI for CN versus CF coupling
A catalyst-controlled selective functionalization of 8-aminoquinolines with N-fluorobenzenesulfonimide (NFSI) has been developed. The use of GTP-Cu catalysts leads to CN coupling products and whereas the CF coupling reaction is dominant for GPT-Ni ...
Kai Zheng +6 more
doaj +1 more source
Aminoquinolines afford resistance to cerebral malaria in susceptible mice
Objectives: Malaria treatment is impeded by increasing resistance to conventional antimalarial drugs. Here we explored the activity of ten novel benzothiophene, thiophene and benzene aminoquinolines. Methods: In vitro testing was performed by the lactate
Jelena Srbljanović +8 more
doaj +1 more source
KAI407, a potent non-8-aminoquinoline compound that kills Plasmodium cynomolgi early dormant liver stage parasites in vitro. [PDF]
Preventing relapses of Plasmodium vivax malaria through a radical cure depends on use of the 8-aminoquinoline primaquine, which is associated with safety and compliance issues.
Borboa, Rachel +25 more
core +1 more source
Background Plasmodium vivax malaria elimination can only be achieved by the deployment of 8-aminoquinolines (primaquine and tafenoquine) in combination with ACT to kill both blood and liver-stage parasites.
Germana Bancone +25 more
doaj +1 more source
Putative Contribution of 8-Aminoquinolines to Preventing Recrudescence of Malaria
Enhanced therapeutic efficacy achieved in treating Plasmodium vivax malaria with an 8-aminoquinoline (8-AQ) drug such as primaquine (PQ) together with a partner drug such as chloroquine (CQ) is usually explained as CQ inhibiting asexual parasites in the ...
Miles B. Markus
doaj +1 more source
Synthesis and Antimycobacterial Evaluation of N-(4-(Benzyloxy)benzyl)-4-aminoquinolines
Tuberculosis remains a global health problem that affects millions of people around the world. Despite recent efforts in drug development, new alternatives are required.
Estevão Silveira Grams +13 more
doaj +1 more source
Cu(II) and Fe(III) complexes of sulphadoxine mixed with pyramethamine: Synthesis, characterization, antimicrobial and toxicology study [PDF]
Two new mixed ligands metal complexes of sulphadoxine and pyramethamine were prepared by using CuCl2.6H2O and FeCl3.6H2O. The complexes were characterized by elemental analysis, melting point determination, molar conductivity, metal content analysis (AAS)
Adekoya, J. A. +5 more
core +4 more sources
Primaquine for Plasmodium vivax radical cure: What we do not know and why it matters
Plasmodium vivax radical cure requires the administration of a blood schizonticide for killing blood-stage parasites and the addition of a drug able to kill hypnozoites, the dormant parasite stages residing in the liver of infected patients.
Jean Popovici +3 more
doaj +1 more source
A first example of cobalt-catalyzed remote C-H functionalization of 8-aminoquinolines operating through a single electron transfer mechanism [PDF]
The development of new C[BOND]H functionalization protocols based on inexpensive cobalt catalysts is currently attracting significant interest. Functionalized 8-aminoquinoline compounds are high-potential building blocks in organic chemistry and ...
Ackermann +49 more
core +1 more source
Primaquine-induced haemolysis in females heterozygous for G6PD deficiency
Oxidative agents can cause acute haemolytic anaemia in persons with G6PD deficiency. Understanding the relationship between G6PD genotype and the phenotypic expression of the enzyme deficiency is necessary so that severe haemolysis can be avoided.
Cindy S. Chu +4 more
doaj +1 more source

