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9. What is the significance structure of a drug as far as drug design is concerned? 10. Outline why the stereochemistry of a compound is important in drug design 11. Outline by means of suitable examples what the significance of (a) structurally rigid groups, (b) conformations and(c)configuration has on the design of new drugs 12. Why is water solubility an important factor in the action of drugs? 13. Define the meaning of the terms: (a)ideal solution and(b) polar solute 14. List the structural features that would indicate whether a compound is likely to be reasonably ater soluble Illustrate the answer by reference to suitable examples 15. Outline three general methods by which the water solubility of a compound could be improved without affecting its type of biological action 16. Suggest, by means of chemical equations, one route for the introduction of each of the following residues into the structure of 4-hydroxybenzenesulphonamide (a) an acid residue (b)a basic residue (c)a neutral polyhydroxy residue 17. State the full wording of the abbreviation"SAR" Describe the general way in which SAr is ed to develop a drug 18.(a) Explain why chloride and fluorine are normally the preferred halogen substituents for a SAR Investigation (b) What alternative halogen containing group could be used in place of chlorine? Give one reason for the use of this group 19. Explain the meaning of the terms:(a) bioisostere and(b) pharmacophore 20. Suggest how the introduction of each of the following groups into the structure of a lead could be expected to affect the pharmacokinetics of the resultant analogue:(a) a sulphonic acid group, (b) a methyl group and (c)a thiol group. Assume that these groups are introduced into the section of the lead, structure that does not contain its pharmacophore9. What is the significance structure of a drug as far as drug design is concerned? 10. Outline why the stereochemistry of a compound is important in drug design. 11. Outline by means of suitable examples what the significance of (a) structurally rigid groups, (b) conformations and (c) configuration has on the design of new drugs. 12. Why is water solubility an important factor in the action of drugs? 13. Define the meaning of the terms: (a) ideal solution and (b) polar solute 14. 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. 15. Outline three general methods by which the water solubility of a compound could be improved without affecting its type of biological action. 16. Suggest, by means of chemical equations, one route for the introduction of each of the following residues into the structure of 4-hydroxybenzenesulphonamide. (a) an acid residue (b) a basic residue (c) a neutral polyhydroxy residue. 17. State the full wording of the abbreviation “SAR”. Describe the general way in which SAR is used to develop a drug. 18. (a) Explain why chloride and fluorine are normally the preferred halogen substituents for a SAR investigation. (b) What alternative halogen containing group could be used in place of chlorine? Give one reason for the use of this group. 19. Explain the meaning of the terms: (a) bioisostere and (b) pharmacophore. 20. Suggest how the introduction of each of the following groups into the structure of a lead could be expected to affect the pharmacokinetics of the resultant analogue: (a) a sulphonic acid group, (b) a methyl group and (c) a thiol group. Assume that these groups are introduced into the section of the lead, structure that does not contain its pharmacophore
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