One of these ways consists of reacting 3-chloroaniline with ethoxymethylenmalonic ester to make (3-choroanilino)-methylenemalonic ester (18.104.22.168), which then undergoes high-temperature heterocyclization to make the ethyl ester of 7-chloro-4-hydroxyquinolin-3-carboxylic acid (22.214.171.124). Hydrolyzing this with sodium hydroxide gives 7-chloro-4-hydroxyquinolin-3-decarboxylic acid (126.96.36.199), which when heated at 250–270 C is decarboxylated, forming 7-chloro-4-hydroxyquinoline (188.8.131.52). G6pd deficiency hydroxychloroquine Side effects plaquenil tablets Plaquenil indication apl syndrome The clinical usefulness of chloroquine, and in some recent cases of quinine as well, has been much reduced by the evolution and spread of chloroquine resistant malaria parasites. The mechanism of resistance involves a reduced accumulation of the drug, although again the mechanism involved is controversial. Chloroquine 4-Aminoquinoline derivatives Uncharged at neutral pH Diffuse freely into lysosome of parasite At acid pH of lysosome, it converted to a protonated, membrane impermeable form and is ‘trapped’ inside the parasite. At high conc. It inhibits protein RNA and DNA synthesis. 13 14. Chloroquine is the drug of choice for preventing and treating acute forms of malaria caused by P. vivax, P. malariae, P. ovale, as well as sensitive forms of P. mechanism of its action is not completely clear, although there are several hypotheses explaining its antimalarial activity. Alkaline hydrolysis of the ethyl ester of the 7-chloro-4-hydroxyquinolin-2-carboxylic acid (184.108.40.206) and subsequent high-temperature decarboxylation of the resulting acid (220.127.116.11) gives 7-chloro-4-hydroxyquinolin (18.104.22.168). Treating this with phosphorus oxychloride gives one of the desired components for synthesis of chloroquine – 4,7-dichloroquinoline (22.214.171.124) [The second method of preparing of 4,7-dichloroquinoline (126.96.36.199) consists of reacting 3-chloroaniline with the diethyl ester of oxaloacetic acid in the presence of acetic acid to give the corresponding enamine (188.8.131.52), which when heated to 250 °C undergoes heterocyclization to the ethyl ester of 7-chloro-4-hydrozyquinolin-2-carboxylic acid (184.108.40.206) accompanied with a small amount of 5-chloro-4-hydroxyquinolin-2-carboxylic acid (220.127.116.11), which is separated from the main product by crystallization from acetic acid. Synthesis of chloroquine phosphate slideshare General Preparation - Chloroquine Phosphate Injection., Antimalarial agents - pt. Plaquenil sjorensHydroxychloroquine sulfate tabletsPlaquenil crpPrice hydroxychloroquineHydroxychloroquine toxic retinopathy Chloroquine is a synthetic aminoquinoline that acts by binding to the protozoal or parasitic DNA and preventing DNA and RNA production and subsequent protein synthesis; it is active against the asexual erythrocytic forms of Plasmodium and Entamoeba species. Chloroquine - LiverTox - NCBI Bookshelf. Chloroquine - an overview ScienceDirect Topics. Pharmacology of Chloroquine - YouTube. Glycerophospholipids They are the major lipids that occur in biological membranes They consist of glycerol-3-phosphate esterified at its C1 and C2 with fatty acids Phosphatidic acid This is simplest phospholipids Does not occur in good concentration in tissues It is an intermediate in the synthesis of TAG and phospholipids Chloroquine Phosphate is the phosphate salt of chloroquine, a quinoline compound with antimalarial and anti-inflammatory properties. Chloroquine is the most widely used drug against malaria, except for those cases caused by chloroquine resistant Plasmodium falciparum. Although the mechanism of action is not fully understood, chloroquine is shown to inhibit the parasitic enzyme heme polymerase. Among the antimalarial drugs chloroquine is commonly used. • Pyrimethamine, sulfones, & tetracyclines are slower acting, less effective, & nearly always used in combination with other antimalarial drugs • The artemisinins are potent and fast-acting antimalarials with no clinical evidence of resistance.