Chloroquine based chalcone

Discussion in 'Reliable Pharmacy' started by barz, 22-Feb-2020.

  1. Zwerty User

    Chloroquine based chalcone

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    A series of hybrids made of 4-chlorochalcone 17, and the antimalarial drug chloroquine 18 were designed and tested for their antimalarial efficacy against chloroquine-resistant strain K1 of. The preparation of amide based chloroquine-chalcone analogues 18–22, which were obtained by the combination of amido chloroquine 17 and aldehydes in 10% aq. KOH in methanol at room temperature. The amido chloroquine 17 was prepared from acid 16 and compound 2 in benzene using SOCl2 as chlorinating agent. The compounds were screened for their antimalarial activity. Two chalcones, five benzylidenesulfonamides and three chalconesulfonamides showed antimalarial activity equivalent to chloroquine.

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    Chloroquine based chalcone

    Potent antimalarial activity of newly synthesized., Cinnamoylated chloroquine analogues A new structural class.

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  7. Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum Article in Bioorganic & medicinal chemistry letters 22175455.

    • Synthesis and in vitro evaluation of new chloroquine-chalcone..
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    Dec 16, 2019 The anti-malarial property of chalcone was first reported after an in vitro evaluation of an oxygenated chalcone, “licochalcone A” exclusively obtained from Chinese licorice, as an anti-malarial agent against chloroquine sensitive and chloroquine resistant Plasmodium strains. The chloroquine-based hybrids were less active blood schizonticidal drugs against 3D7 and FCR-3 strains. The poor antimalarial activity of primaquine-based hybrids is due to the resistance-reversing effect of primaquine. Jul 25, 2017 Chloroquine interferes with the parasite detoxification process by inhibiting heme transformation into hemozoin. The accumulation of heme causes severe damage to the parasite, leading to its death 58,59. The antimalarial property of chalcone derivatives is derived from their ability to inhibit the parasitic cysteine proteases, such as falcipain.

  8. maks3000 Guest

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  9. LILIADU Well-Known Member

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  10. Nightbear XenForo Moderator

    Mechanisms of Other Antimicrobial Drugs Microbiology Quinolines are thought to interfere with heme detoxification, which is necessary for the parasite’s effective breakdown of hemoglobin into amino acids inside red blood cells. The synthetic derivatives chloroquine, quinacrine also called mepacrine, and mefloquine are commonly used as antimalarials, and chloroquine is also used to treat amebiasis typically caused by Entamoeba histolytica.

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