PPT NO. 2 - Introduction to Medicinal Chemistry PDF

INTRODUCTION TO MEDICINAL CHEMISTRY PPT NO. 2 (DR. GUPTA) 1. What is the significance of medicinal chemistry in pharmacy education? A: It helps understand the structure, interactions, and properties of drugs. 2. What can a medicinal chemist determine for a drug molecu...

INTRODUCTION TO MEDICINAL CHEMISTRY PPT NO. 2 (DR. GUPTA) 1. What is the significance of medicinal chemistry in pharmacy education? A: It helps understand the structure, interactions, and properties of drugs. 2. What can a medicinal chemist determine for a drug molecule? A: Functional groups, interactions with biological targets, acid/base character, polarity, and solubility. 3. What does SAR stand for in medicinal chemistry? A: Structure-Activity Relationship. 4. What is a pharmacophore? A: Essential structural features of a drug responsible for biological activity. 5. How does solubility relate to drug action? A: Solubility affects drug absorption, distribution, and bioavailability. 6. Name two disciplines that medicinal chemistry combines. A: Biology and pharmaceutical sciences. 7. What are the ADME properties in drug development? A: Absorption, Distribution, Metabolism, and Excretion. 8. How does the polarity of a drug affect its solubility? A: Polar drugs are water-soluble; non-polar drugs are lipid-soluble. 9. What is the partition coefficient (logP) used for? A: To measure the polarity of a drug between water and lipid environments. 10. What is the role of hydrogen bonding in drug-receptor interactions? A: It stabilizes the interaction between the drug and receptor. 11. Why must a drug balance hydrophilicity and lipophilicity? A: To cross biological membranes while remaining soluble in bodily fluids. 12. What types of functional groups increase water solubility? A: Polar and ionizable groups like hydroxyl and amine groups. 13. What is the effect of alkyl chains on drug solubility? A: They increase lipophilicity and decrease water solubility. 14. What is the purpose of studying the acidity and basicity of drugs? A: To predict solubility and ionization in different pH environments. 15. Which functional group is basic: amine or carboxylic acid? A: Amine. 16. How does the Henderson-Hasselbalch equation relate to drug ionization? A: It calculates the ionization state of drugs at different pH values. 17. What does a high logP indicate about a drug’s solubility? A: It is more lipophilic and less water-soluble. 18. What is the main goal of drug design in medicinal chemistry? A: To achieve the desired therapeutic effect with minimal side effects. 19. What are common acidic functional groups in drugs? A: Carboxylic acids and phenols. 20. What role do Van der Waals forces play in drug binding? A: They help drugs fit within receptor binding sites. 21. Define an amphoteric compound. A: A compound with both acidic and basic functional groups. 22. Why is understanding drug reactivity important? A: It influences the drug’s stability and potential interactions. 23. What does SAR study in drug molecules? A: The relationship between chemical structure and biological activity. 24. Why are functional groups critical in drug design? A: They determine a drug’s solubility, reactivity, and binding interactions. 25. What is a prodrug? A: A compound that requires activation within the body to become pharmacologically active. 26. Give an example of a prodrug. A: Atorvastatin. 27. How does drug ionization affect absorption? A: Ionized drugs are less permeable across lipid membranes. 28. What is the significance of ADME in pharmacokinetics? A: It determines how the drug is processed in the body. 29. What is the primary functional group in morphine’s pharmacophore? A: An aromatic ring with a protonated amine and hydrophobic region. 30. How do lipophilic drugs interact with membranes? A: They diffuse through lipid bilayers more readily. 31. Why are hydroxyl groups important for solubility? A: They enhance water solubility due to hydrogen bonding. 32. What does a low logP value suggest? A: The drug is more hydrophilic and water-soluble. 33. What is an example of a nonpolar functional group? A: Alkyl chains. 34. What does drug polarity impact besides solubility? A: Membrane permeability and distribution. 35. What is the pharmacophore of statins? A: The structure responsible for inhibiting cholesterol synthesis. 36. What is the difference between organic and medicinal chemistry? A: Organic chemistry studies molecules; medicinal chemistry focuses on their therapeutic uses. 37. How do functional groups like nitro groups affect logP? A: They decrease logP, increasing hydrophilicity. 38. What are macromolecular drug targets? A: Receptors, enzymes, and DNA/RNA. 39. Define “efficacy” in medicinal chemistry. A: The ability of a drug to produce the desired therapeutic effect. 40. What happens to drug solubility as acidity increases? A: Solubility in water increases for acidic drugs. 41. Why do drugs with balanced solubility have an advantage? A: They can move through both aqueous and lipid environments effectively. 42. What is a hydrophobic region’s role in a pharmacophore? A: It enhances binding with lipophilic regions of receptors. 43. How does polarity affect drug distribution? A: Polar drugs remain in aqueous compartments, while nonpolar drugs enter lipid tissues. 44. Why is SAR important in drug design? A: It helps optimize drug efficacy and reduce side effects. 45. What is the function of hydrogen bonds in drug action? A: They stabilize drug-receptor interactions. 46. Define “bioavailability” in pharmacology. A: The extent and rate at which a drug reaches systemic circulation. 47. What is a hydrophilic drug characteristic? A: It dissolves easily in water and circulates in bodily fluids. 48. How does a drug’s structure affect its metabolism? A: Functional groups can alter enzyme interactions and breakdown rates. 49. What does ionization depend on? A: The drug’s pKa and the pH of the environment. 50. Why are quaternary ammonium compounds neutral at physiological pH? A: They do not ionize in water. 51. Why do lipophilic drugs have higher logP values? A: They have a greater affinity for lipid over aqueous phases. 52. What type of bonding is common in drug-receptor interactions? A: Ionic, hydrogen, covalent, and Van der Waals interactions. 53. Why is polarity crucial for drug transport? A: Nonpolar drugs cross membranes more easily than polar ones. 54. What is the impact of adding polar groups to a molecule? A: It increases hydrophilicity and decreases lipophilicity. 55. What does an aromatic ring contribute to a drug? A: It provides stability and a hydrophobic region for binding. 56. How does lipophilicity relate to drug toxicity? A: Highly lipophilic drugs may accumulate in lipid tissues, increasing toxicity risk. 57. What is the advantage of a drug being amphoteric? A: It can exist in both acidic and basic forms, adjusting to pH changes. 58. What is the significance of functional group chemistry? A: It determines solubility, reactivity, and pharmacological interactions. 59. How does pH affect weak acid and base drugs? A: Changes in pH alter their ionization and, consequently, their solubility and absorption. 60. What are the therapeutic implications of a drug's solubility? A: Solubility affects how a drug is formulated, administered, and absorbed. 61. Why is chemical bonding essential for drug-receptor fit? A: It enables drugs to bind specifically and tightly to their targets. 62. What effect does adding alkyl groups have on a drug molecule? A: It increases lipophilicity, making it more likely to bind to lipids. 63. How can SAR studies guide drug modification? A: They show how changes in structure impact drug activity. 64. What are the primary types of functional groups in drugs? A: Alcohols, amines, carboxylic acids, and esters. 65. What is the role of the aromatic ring in morphine? A: It is part of its pharmacophore, essential for receptor binding. 66. Define “bioisosteres” in medicinal chemistry. A: Groups or atoms with similar properties used to modify drugs while retaining activity. 67. How do enzymes affect drug metabolism? A: They break down drugs, affecting duration and potency. 68. What is the role of hydrophilic groups in drug design? A: They improve solubility and distribution in water-based fluids. 69. Why do we study acid-base properties in drug formulation? A: They influence the drug’s solubility, stability, and absorption. 70. What does the term “protonated amine” refer to in pharmacophores? A: An amine group with an added hydrogen ion, aiding in receptor binding. 71. How do functional groups affect the logP value? A: Polar groups decrease logP, making the drug more hydrophilic. 72. Why are covalent bonds uncommon in drug-receptor interactions? A: They are often too strong and irreversible, limiting drug use. 73. What does “hydrophilic-lipophilic balance” mean in drug design? A: It is the right mix of water and lipid solubility for optimal drug action. 74. How does ionization state affect drug bioavailability? A: Un-ionized drugs are absorbed better through membranes. 75. What effect does an ester functional group have on a drug? A: It can improve lipophilicity and membrane permeability. 76. How does a high logP value affect oral bioavailability? A: It may reduce solubility and thus limit absorption in the GI tract. 77. What does a functional group’s presence indicate about solubility? A: Polar groups suggest higher solubility in water. 78. How does pH-dependent ionization influence drug excretion? A: Ionized drugs are less likely to be reabsorbed, increasing excretion. 79. What is the pharmacophore of a drug? A: Structural features essential for biological activity. 80. What does “hydrophobic” mean? A: Water-repelling, often associated with lipid solubility. 81. How does drug solubility affect its route of administration? A: Soluble drugs are easier to formulate for oral or injectable use. 82. What is the role of basic functional groups in drug absorption? A: They interact with acidic environments for enhanced absorption. 83. Why is understanding polarity crucial for drug development? A: It affects solubility, distribution, and receptor binding. 84. How do aromatic amines influence drug structure? A: They add both hydrophobicity and potential for ionization. 85. Why are lipophilic drugs effective in crossing membranes? A: They can dissolve in the lipid bilayer. 86. How does the physicochemical property of a drug impact its ADME profile? A: It influences absorption, distribution, metabolism, and excretion. 87. What does an “acidic drug” mean? A: A drug with a functional group that donates protons in solution. 88. What is the relationship between drug structure and receptor interaction? A: Structure dictates affinity and effectiveness of the interaction. 89. How does solubility affect drug onset and duration? A: Soluble drugs act faster but may have shorter durations. 90. Why are bioisosteric modifications used in drug design? A: To alter drug properties without losing activity. 91. How does polarity affect the drug’s pharmacokinetic properties? A: Nonpolar drugs may distribute more in lipid-rich areas. 92. What is the benefit of a balanced solubility in drugs? A: It supports absorption in aqueous and lipid environments. 93. How does a drug’s molecular size affect its absorption? A: Smaller molecules diffuse more easily across membranes. 94. What is an example of a highly polar functional group? A: Hydroxyl group (-OH). 95. Why is lipophilicity important in drugs for brain penetration? A: Lipophilic drugs cross the blood-brain barrier more effectively. 96. How do electron-donating groups affect acidity? A: They decrease acidity by stabilizing the molecule. 97. What is the function of an ether group in a drug? A: It can increase lipid solubility without adding polarity. 98. How do alkanes affect a molecule’s overall logP? A: They increase logP, enhancing lipophilicity. 99. Why is water solubility essential for intravenous drugs? A: It ensures they can be dissolved and administered in solution. 100. How does the presence of nitrogen affect drug structure? A: It can introduce basicity and improve binding with acidic targets.