3.7 Questions
(1) Outline the general steps in the discovery of a new drug.
(2) Outline by means of suitable examples the significance of (i) structurally rigid
groups, (ii) conformations and (iii) configuration on the design of new drugs.(3) Explain why water solubility is an important factor in drug design.
(4) List the structural features that would indicate whether a compound is likely
to be reasonably water soluble. Illustrate the answer by reference to suitable
examples.(5) Suggest general methods by which the water solubility of a compound could
be improved without affecting its type of biological action.(6) Suggest, by means of chemical equations, one route for the introduction of
each of (i) an acid residue and (ii) a basic residue into the structure of
4-hydroxybenzenesulphonamide when the sulphonamide group acts as the
pharmacophore in this compound.70 AN INTRODUCTION TO DRUG DISCOVERY