Pharmaceutical Lead Compound Identification and Optimization

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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?

Retaining the activity and avoiding patent restrictions Signup and view all the answers

What is the difference between extensive screening and random screening?

Extensive screening involves a large number of biological targets, while random screening involves a limited number of experimental models Signup and view all the answers

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

Screening thousands of compounds on a large number of biological targets Signup and view all the answers

Which antihistaminics were introduced in 1980 to reduce sedation?

Istemizole and terfenadine Signup and view all the answers

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

Amines derived from phenothiazine Signup and view all the answers

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

To identify one or more lead compounds Signup and view all the answers

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

To reduce the patent restrictions on the compound Signup and view all the answers

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

The lead compound has more undesirable side effects Signup and view all the answers

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

A large number of compounds are tested on a limited number of biological targets Signup and view all the answers

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

It allows for the testing of a larger number of compounds Signup and view all the answers

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

Reducing sedation Signup and view all the answers

What is the primary goal of a lead optimization process?

To improve the pharmacokinetic and pharmacodynamic properties of a lead compound Signup and view all the answers

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

The daily dose of the compound is reduced Signup and view all the answers

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

To avoid legal issues with the patent holder Signup and view all the answers

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

It increases the chances of discovering a new drug Signup and view all the answers