Antituberculosis Drugs: Chemistry and Synthesis Quiz
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Questions and Answers

What is the primary use of Isoniazid?

  • Prophylaxis against tuberculosis in high-risk individuals
  • Treatment of drug-resistant tuberculosis
  • Treatment of active tuberculosis caused by susceptible strains (correct)
  • Treatment of latent tuberculosis infection

    • Which structural feature of Isoniazid is essential for its anti-tuberculosis activity?

  • The unsubstituted nitrogen at N1
  • The pyridine ring (correct)
  • The carbonyl group
  • The carbohydrazine group

    • Which of the following is a second-line anti-tuberculosis drug?

  • Ethambutol
  • Isoniazid
  • Rifampicin
  • Ethionamide (correct)

    • What is the primary purpose of using Streptomycin in combination with other anti-TB drugs?

    <p>To prevent the development of drug resistance</p> Signup and view all the answers

    Which of the following is NOT a first-line anti-tuberculosis drug?

    <p>Amikacin</p> Signup and view all the answers

    What is the primary structural modification that distinguishes Ethionamide from Isoniazid?

    <p>Substitution of the carbonyl group with a thiocarbonyl group</p> Signup and view all the answers

    What is the waxy coating on the cell surface of Mycobacterium tuberculosis primarily due to?

    <p>Presence of mycolic acid</p> Signup and view all the answers

    Why did resistance occur rapidly with the first anti-TB drug, sulfanilamide?

    <p>It was bacteriostatic</p> Signup and view all the answers

    What was the major breakthrough in TB treatment regarding antibiotics?

    <p>Development of streptomycin</p> Signup and view all the answers

    What characteristic of Mycobacterium tuberculosis makes most antibiotics ineffective against it?

    <p>Presence of a waxy coating</p> Signup and view all the answers

    Why was dapsone discontinued in long-term TB therapy despite its effectiveness?

    <p>It was toxic</p> Signup and view all the answers

    Which bacterium causes TB and is known as Koch's bacillus?

    <p>Mycobacterium tuberculosis</p> Signup and view all the answers

    What is the effect of substituting N with C in the pyrazine ring?

    <p>It results in a decrease in activity</p> Signup and view all the answers

    What is the mode of action of pyrazinamide?

    <p>Pyrazinamide is a prodrug that is activated by M. tuberculosis amidase enzyme into pyrazine carboxylic acid, which has bactericidal activity</p> Signup and view all the answers

    What is the main cause of resistance to pyrazinamide?

    <p>Decreased uptake of pyrazinamide by M. tuberculosis</p> Signup and view all the answers

    What is the therapeutic use of pyrazinamide?

    <p>Pyrazinamide is used in conjunction with isoniazid and rifampin in short-course (6-month) regimens for the treatment of tuberculosis</p> Signup and view all the answers

    What are the major adverse effects of pyrazinamide?

    <p>Hepatotoxicity, nausea, vomiting, and hyperuricemia</p> Signup and view all the answers

    Which of the following statements about ethambutol is correct?

    <p>Ethambutol is a synthetic, water-soluble, heat-stable compound that is included in first-line therapy of tuberculosis due to its efficacy and less adverse effects</p> Signup and view all the answers

    Which of the following statements is true about Isoniazid?

    <p>It inhibits the synthesis of mycolic acids, which are essential components of mycobacterial cell walls.</p> Signup and view all the answers

    What is the mode of action of Isoniazid?

    <p>It forms a covalent complex with an acyl carrier protein (AcpM) and KasA, blocking mycolic acid synthesis.</p> Signup and view all the answers

    Which of the following statements is true about Pyrazinamide?

    <p>It has an amide group at position 2 of the pyrazine ring.</p> Signup and view all the answers

    What is the importance of the amide side chain in Pyrazinamide?

    <p>It is essential for the antimycobacterial activity.</p> Signup and view all the answers

    Which of the following statements is true about the clinical application of Isoniazid?

    <p>It is used in combination therapy for active tuberculosis infections.</p> Signup and view all the answers

    Which structural feature of Pyrazinamide is essential for its antimycobacterial activity?

    <p>The presence of a pyrazine ring with two nitrogen atoms.</p> Signup and view all the answers

    What is the primary role of nitrogen atoms in acetazolamide?

    <p>Enhancing the drug's binding affinity through hydrogen bonding and electrostatic interactions with the enzyme</p> Signup and view all the answers

    How does the electronegativity of atoms in acetazolamide affect its properties?

    <p>It affects bonding interactions, impacting the drug's affinity for the enzyme</p> Signup and view all the answers

    What is the purpose of modifying functional groups in acetazolamide?

    <p>To change the drug's properties, including solubility</p> Signup and view all the answers

    What is the effect of adding a methyl group to the ring's nitrogen in acetazolamide?

    <p>It enhances the drug's diuretic activity</p> Signup and view all the answers

    What is a requirement for the moiety attached to the sulfamoyl group in acetazolamide?

    <p>It must possess aromatic character</p> Signup and view all the answers

    Which statement about furosemide is correct?

    <p>It is classified as a high ceiling diuretic</p> Signup and view all the answers

    Study Notes

    Isoniazid

    • The primary use of Isoniazid is as an anti-tuberculosis drug.
    • The structural feature essential for its anti-tuberculosis activity is the hydrazide group.
    • Isoniazid is a first-line anti-tuberculosis drug.

    Other Anti-TB Drugs

    • Ethionamide is a second-line anti-tuberculosis drug.
    • Streptomycin is used in combination with other anti-TB drugs to prevent the development of resistance.
    • Dapsone is not a first-line anti-tuberculosis drug.

    Ethionamide

    • The primary structural modification that distinguishes Ethionamide from Isoniazid is the replacement of the hydrazide group with an ethyl group.
    • Ethionamide is used as a second-line anti-tuberculosis drug.

    Mycobacterium Tuberculosis

    • The waxy coating on the cell surface of Mycobacterium tuberculosis is primarily due to mycolic acid.
    • The bacterium causes TB and is known as Koch's bacillus.
    • The characteristic that makes most antibiotics ineffective against Mycobacterium tuberculosis is its waxy cell wall.

    Pyrazinamide

    • The effect of substituting N with C in the pyrazine ring converts pyrazinamide to a non-anti-tuberculosis compound.
    • The mode of action of pyrazinamide involves the conversion of pyrazinamide to pyrazinoic acid, which then inhibits fatty acid synthase.
    • The main cause of resistance to pyrazinamide is the mutation of the pyrazinamidase gene.
    • The therapeutic use of pyrazinamide is as an anti-tuberculosis drug, particularly in combination with other drugs.
    • The major adverse effects of pyrazinamide include hepatotoxicity and hyperuricemia.

    Ethambutol

    • Ethambutol is used in combination with other anti-TB drugs to prevent the development of resistance.

    Acetazolamide

    • The primary role of nitrogen atoms in acetazolamide is to enhance its diuretic properties.
    • The electronegativity of atoms in acetazolamide affects its properties by increasing its solubility.
    • The purpose of modifying functional groups in acetazolamide is to enhance its diuretic properties.
    • The requirement for the moiety attached to the sulfamoyl group in acetazolamide is that it should be able to enhance its diuretic properties.

    Furosemide

    • Furosemide is a diuretic that works by inhibiting the Na+/K+/2Cl- symporter in the kidneys.

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    Description

    Test your knowledge on the chemistry and synthesis of antituberculosis drugs, particularly those used in combination with trimethoprim (cotrimoxazole). Explore the synthesis of 3-amino 5-methyl isoxazole, P-amino benzene sulfonyl chloride, and more. Learn about the classification, structure-activity relationship (SAR), and uses of antituberculosis drugs.

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