2022-11-12T08:24:19+03:00[Europe/Moscow] en true <p>to get more active, potent, and safer agents</p>, <p>Homologation</p>, <p>9; low water solubility, low bioavailability </p>, <p>Homologation</p>, <p>chain branching; lower lipophilicity, weaker binding with target</p>, <p>ring chain transformation; affects lipophilicity and metabolism</p>, <p>Phenylalanine (PEA)</p>, <p>catecholamine-releasing properties; competes with dopamine and norepinephrine </p>, <p>serotonin 5-HT, SERT, MAO</p>, <p>sulfa, antimicrobial agent, p-amino group, amides; can be converted to prodrugs</p>, <p>competitive inhibitors of DHPS; enzyme essential for folate synthesis </p>, <p>Sulfmethoxazole </p>, <p>6-phosphate dehydrogenase</p> flashcards
CH.6 - Structure-Activity and Structure- Property Relationship Studies

CH.6 - Structure-Activity and Structure- Property Relationship Studies

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  • to get more active, potent, and safer agents

    What is the main aim of structure-activity relationships (SARs)?

  • Homologation

    -lengthen alkyl chain in chemical structure by CH2

  • 9; low water solubility, low bioavailability

    What is the maximum chain length?

    What happens when you exceed this number?

  • Homologation

    What SAR is this?

    What SAR is this?

  • chain branching; lower lipophilicity, weaker binding with target

    What SAR is this? What kind of implications are associated with it?

    What SAR is this? What kind of implications are associated with it?

  • ring chain transformation; affects lipophilicity and metabolism

    What SAR is this? What kind of implications are associated with it?

    What SAR is this? What kind of implications are associated with it?

  • Phenylalanine (PEA)

    -especially high or low concentrations of it is associated with specific psych disorders like ADHD

  • catecholamine-releasing properties; competes with dopamine and norepinephrine

    What structure of Amphetamine is responsible for its psychostimulant effects?

  • serotonin 5-HT, SERT, MAO

    What are the targets for Amphetamine?

  • sulfa, antimicrobial agent, p-amino group, amides; can be converted to prodrugs

    Drug class?Indication?What is essential to its activity?Any exceptions?

    Drug class?

    Indication?

    What is essential to its activity?

    Any exceptions?

  • competitive inhibitors of DHPS; enzyme essential for folate synthesis

    MOA for Sulfonamide antibacterials?

  • Sulfmethoxazole

    -used for the treatment of infections such as

    - chronic bronchitis

    -UTI and ear infections

    -enteric infections, shigellosis, and traveler's diarrhea

    -Pneumocystis pneumonia

  • 6-phosphate dehydrogenase

    Primaquine, an anti-malarial drug, is toxic for individuals who are deficient in

    _______.