Pharmaceutical Lead Compound Identification and Optimization
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Questions and Answers

What is the main characteristic of a lead compound?

  • It has optimal pharmacokinetic properties
  • It has the desired pharmaceutical activity (correct)
  • It is synthesized from a natural source
  • It has no side effects

What is the primary purpose of a drug discovery program?

  • To improve the pharmacodynamic properties of a lead compound
  • To eliminate all side effects of a lead compound
  • To identify a lead compound with optimal pharmacokinetic properties
  • To discover a new drug through a series of programmed searches (correct)

What is the purpose of lead optimization?

  • To eliminate patent restrictions
  • To reduce the daily dose of a lead compound
  • To improve the therapeutic properties of a lead compound (correct)
  • To modify the structure of a lead compound

What is the outcome of modifying the structure of a lead compound?

<p>Retaining the activity and avoiding patent restrictions (B)</p> Signup and view all the answers

What is the difference between extensive screening and random screening?

<p>Extensive screening involves a large number of biological targets, while random screening involves a limited number of experimental models (D)</p> Signup and view all the answers

What is the outcome of combining the two approaches of extensive and random screening?

<p>Screening thousands of compounds on a large number of biological targets (B)</p> Signup and view all the answers

Which antihistaminics were introduced in 1980 to reduce sedation?

<p>Istemizole and terfenadine (D)</p> Signup and view all the answers

Which of the following is an example of a drug that underwent extensive screening?

<p>Amines derived from phenothiazine (A)</p> Signup and view all the answers

What is the purpose of a drug discovery program's first task?

<p>To identify one or more lead compounds (B)</p> Signup and view all the answers

What is the primary goal of modifying a lead compound's structure?

<p>To reduce the patent restrictions on the compound (A)</p> Signup and view all the answers

What is the primary difference between a lead compound and a fully optimized drug?

<p>The lead compound has more undesirable side effects (C)</p> Signup and view all the answers

Which of the following is a characteristic of a random screening approach?

<p>A large number of compounds are tested on a limited number of biological targets (C)</p> Signup and view all the answers

What is the primary advantage ofcombining extensive and random screening approaches?

<p>It allows for the testing of a larger number of compounds (A)</p> Signup and view all the answers

Which of the following is an example of a pharmaceutical activity that may be improved during lead optimization?

<p>Reducing sedation (D)</p> Signup and view all the answers

What is the primary goal of a lead optimization process?

<p>To improve the pharmacokinetic and pharmacodynamic properties of a lead compound (A)</p> Signup and view all the answers

What is the outcome of improving the pharmacokinetic properties of a lead compound?

<p>The daily dose of the compound is reduced (D)</p> Signup and view all the answers

What is the primary reason for modifying the structure of a lead compound to avoid patent restrictions?

<p>To avoid legal issues with the patent holder (B)</p> Signup and view all the answers

What is the primary advantage of using a lead compound with a strong pharmaceutical activity?

<p>It increases the chances of discovering a new drug (C)</p> Signup and view all the answers

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