Chloroquine based chalcone

Discussion in 'Northwest Pharmacy Canada' started by fusion2005, 10-Mar-2020.

  1. sexgerl Guest

    Chloroquine based chalcone


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    Sep 05, 2015 Chloroquine-based hybrid molecules as promising novel chemotherapeutic agents Average time to develop a new drug is approximately 12–15 years Meunier, 2008 at an estimated cost of $161 million–$ 1.8 billion USD, depending on the therapeutic areas Morgan et al. 2011. A new series of chloroquinoline based chalcones were synthesized and evaluated for in vitro antiamoebic and antimalarial activities. The results showed that out of fifteen compounds, four were found to be more active against the Entamoeba histolytica; while one compound was moderatively active compared to the standard drug metronidazole IC 50 = 1.46 μM. Molecular docking studies revealed the binding orientation of these chalcones in the active sites of falcipain‐2. Our results clearly depict the advantage of these chalcones as they kill P. falciparum malaria parasite in culture, most likely via inhibition of falcipain.

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    Chloroquine based chalcone

    Chalcone hybrids as privileged scaffolds in antimalarial., Antiprotozoal activity of chloroquinoline based chalcones.

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  3. Amodiaquine is one of the most potent antimalarial 4-aminoquinolines known and remains effective against chloroquine-resistant parasites, but toxicity issues linked to a quinone-imine metabolite limit its clinical use.

    • Synthesis of New 4-Aminoquinolines and Evaluation of Their..
    • In Vitro Antimalarial Evaluation of Piperidine‐ and..
    • Chalcones - an overview ScienceDirect Topics.

    Synthesis and in vitro evaluation of new chloroquine-chalcone hybrids against chloroquine-resistant strain of Plasmodium falciparum Article in Bioorganic & medicinal chemistry letters 22175455. Phenylurenyl chalcone derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-resistant strain of Plasmodium falciparum, activity of the cysteine protease falcipain-2, in vitro globin hydrolysis, β-hematin formation, and murine Plasmodium berghei malaria. The most active antimalarial compound was 1-3‘-N-N‘-phenylurenylphenyl-33,4,5. Chalcone derivatives are well known for their broad spectrum of pharmacological activities, inclusing radical scavenger 9, antihepatotoxic 10, anticancer 11, and antimalarial properties 12. Alkoxylated chalcone derivatives exhibited higher antimalarial activity compared to hydroxylated chalcones 13.

     
  4. ivan-c Well-Known Member

    Plaquenil (hydroxychloroquine) belongs to a group of medicines called quinolines. Hydroxychloroquine Side Effects, Dosage, Uses, and More Protecting your eyesight when taking Plaquenil Lupus. AMANTADINE - ORAL Symmetrel side effects, medical uses.
     
  5. murd User

    Sulfasalazine and Plaquenil drug interactions - eHealthMe Drug interactions are reported among people who take Sulfasalazine and Plaquenil together. This study is created by eHealthMe based on reports of 7,132 people who take Sulfasalazine and Plaquenil from Food and Drug Administration FDA, and is updated regularly. eHealthMe is the source of postmarketing drug monitoring.

    Combination therapy with sulfasalazine and methotrexate is more.