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Antituberculosis Drugs: Chemistry and Synthesis Quiz

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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Questions and Answers

What is the primary use of Isoniazid?

Treatment of active tuberculosis caused by susceptible strains

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

The pyridine ring

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

Ethionamide

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

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