Chloroquine structure activity relationship

Discussion in 'Canada Drug' started by wind-Art, 11-Mar-2020.

  1. Rybak Well-Known Member

    Chloroquine structure activity relationship


    Chloroquine has been extensively used in mass drug administrations, which may have contributed to the emergence and spread of resistance. It is recommended to check if chloroquine is still effective in the region prior to using it.

    Plaquenil ocular screening Chloroquine elimination route

    Abstract. Chloroquine is thought to exert its antimalarial effect by preventing the polymerization of toxic heme released during proteolysis of hemoglobin in the Plasmodium digestive vacuole. The mechanism of this blockade has not been established. We incubated cultured parasites with subinhibitory doses of 3Hchloroquine and 3H quinidine. Chloroquine has a high affinity for tissues of the parasite and is concentrated in its cytoplasm. As a weak base, it increases the pH of the intracellular lysosome and endosome. A more acidic medium in these organelles is needed for the parasite to affect mammalian cells. As a result, chloroquine inhibits growth and development of parasites. Structure-activity relationships SAR explore the relationship between a molecule’s biological activity and the three dimensional structure of the molecule. If the target structure is known, computational chemistry and molecular modelling software packages can be useful in identifying binding site interactions.

    The Centers for Disease Control and Prevention recommend against treatment of malaria with chloroquine alone due to more effective combinations. In areas where resistance is present, other antimalarials, such as mefloquine or atovaquone, may be used instead.

    Chloroquine structure activity relationship

    What is a Structure Activity Relationship SAR?, Chloroquine - an overview ScienceDirect Topics

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  3. Structure-Activity Relationship between Thiol Group-Trapping Ability of Morphinan Compounds with a Michael Acceptor and Anti-Plasmodium falciparum Activities by Noriki Kutsumura 1,2, Yasuaki Koyama 2, Tsuyoshi Saitoh 1, Naoshi Yamamoto 1, Yasuyuki Nagumo 1, Yoshiyuki Miyata 3, Rei Hokari 4, Aki Ishiyama 4, Masato Iwatsuki 4, Kazuhiko.

    • Structure-Activity Relationship between Thiol Group..
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    The structureactivity relationship is the relationship between the chemical structure of a molecule and its biological activity. This idea was first presented by Crum-Brown and Fraser in 1865. The analysis of SAR enables the determination of the chemical group responsible for evoking a target biological effect in the organism. This allows modification of the effect or the potency of a bioactive compound by changing its chemical structure. Medicinal chemists use the techniques of chemical. Dec 24, 2016 Structure Activity Relationship of CHLOROQUINE. Addition of alpha diethylaminocresol in place of diethyl –diamino pentane results in production of amodiaquine, which is less toxics and also less effective as compared to chloroquine. Any substitution at position 1,2,5,6 will lead to decrease the pharmacological activity. Chloroquine enters the red blood cell by simple diffusion, inhibiting the parasite cell and digestive vacuole. Chloroquine then becomes protonated to CQ2+, as the digestive vacuole is known to be acidic pH 4.7; chloroquine then cannot leave by diffusion.

     
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