MO3 Drug lead discovery

Question 1

A drug lead is something [blank_start]likely[blank_end] to be therapeutically useful. It is used as a starting point for [blank_start]chemical modifications[blank_end] to improve potency, selectivity, or pharmacokinetic parameters.

Accepted Answer

likely

Accepted Answer

chemical modifications

Answer

certain

Answer

physical alterations

Question 2

The higher the potency the better.

Answer

true

Question 3

The three broad methods to finding a lead are random screening, synthesis, and direct screening.
[blank_start]Random[blank_end] screening includes screening of synthetic compounds from in house libraries, combinatorial chemistry/parallel synthesis, screening of fragment libraries, and screening of known drugs or natural product libraries. Combinatorial chemistry [blank_start]rapidly[blank_end] generates a large number of structurally related molecules.
[blank_start]Synthesis[blank_end] is also known as "Targeted Drug Discovery" or Rational Design. The Topliss scheme can be followed to find the most appropriate aliphatic [blank_start]substituents[blank_end].
[blank_start]Direct[blank_end] Screening includes endogenous compounds, structure based drug design, virtual screening, and de novo (new) design.

Accepted Answer

Random

Accepted Answer

Direct

Accepted Answer

Synthesis

Accepted Answer

rapidly

Accepted Answer

substituents

Question 4

What is a pharmacophore?

Accepted Answer

The 3D spatial arrangement of groups responsible for a defined biological activity.

Answer

An atom or group whose presence is responsible for the vibrational frequency of a compound.

Answer

A structurally similar isomer.

Question 5

Many new drugs are created by enhancing the side effects of existing drugs.

Answer

true

Question 6

Drug metabolism studies are usually not worthwhile when developing drugs or removing side effects.

Answer

true

MO3 Drug lead discovery

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