Chapter 8 MCQs

* not completed

. Optimisation of the lead compound is carried out in order to attempt to

improve the binding to the drug target. correct incorrect

improve the selectivity for the drug target. correct incorrect

identify the pharmacophore for the drug target. correct incorrect

identify the mechanism of action of the lead compound. correct incorrect

* not completed

. Which of the following structural variations would NOT form part of the SAR guidelines?

Introduction of alkyl halides correct incorrect

Introduction of halogen atoms correct incorrect

Introduction of alkyl groups correct incorrect

Introduction of hydroxyl group correct incorrect

* not completed

. Use of isosterism is the introduction of groups that would be expected that would NOT be expected to produce significant change in

selectivity. correct incorrect

toxicity. correct incorrect

potency. correct incorrect

metabolism. correct incorrect

* not completed

. Which one of the following is NOT a classical isostere?

CONH correct incorrect

Cl correct incorrect

COO correct incorrect

COCH₂ correct incorrect

* not completed

. Which of the following structural changes would NOT be made in order to change the size and shape of a lead compound?

Introduction of a hydroxyl group correct incorrect

Introduction of an aromatic ring correct incorrect

Removal of an aromatic ring correct incorrect

Introduction of extra methylene groups correct incorrect

* not completed

. Which of the following would probably NOT result from the introduction of a new alkyl substituent into a lead compound?

Improved absorption profile of the molecule. correct incorrect

Increased distribution of the molecule. correct incorrect

Decreased lipophilicity of the molecule. correct incorrect

Increased role of oxidative metabolism. correct incorrect

* not completed

. Introduction of which ONE of the following substituents into the lead compound would increase its lipophilicity?

Hydroxy substituent correct incorrect

Amine substituent correct incorrect

Carboxylic acid substituent correct incorrect

Halogen substituent correct incorrect

* not completed

. Which of the following drugs was NOT produced as a result of simplification of a complex natural structure?

Procaine correct incorrect

Morphine correct incorrect

Suxamethonium correct incorrect

Mitoxantrone correct incorrect

* not completed

. Which of the following drugs does NOT exhibit different enantiomeric potencies?

Propranolol correct incorrect

Verapamil correct incorrect

Promethazine correct incorrect

Methyldopa correct incorrect

* not completed

. Which of the following pairs of drugs does NOT show an increased resistance to metabolism?

Tubocurarine ? suxamethonium correct incorrect

Procaine ? lidocaine correct incorrect

Acetylcholine ? carbachol correct incorrect

Benzylpenicillin ? oxacillin correct incorrect