Fundamentals of Medicinal Chemistry and Drug Metabolism

Table of Contents

Chapter 1 Introduction 

• Brief History And Role Of Pharmacists
  
• Brief History Of Medicinal Chemistry
  
• Definition Of Medicinal Chemistry
  
• Medicinal Chemistry In Pharmacy Education
  
• M O Faruk Khan And Ashok Philip
  
• An Abridged Medicinal Chemistry Vocabulary
  
• Medicinal Chemistry In Drug Discovery And Development
  
• Scope Of This Book Series
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• References
  

Chapter 2 Review Of Bioorganic Chemistry 

• M O Faruk Khan And Ashim Malhotra
  
• An Introduction To Organic Functional Groups
  
• Alkanes, Alkenes And Cycloalkanes
  
• Definition And Nomenclature Of Alkanes, Alkenes And Cycloalkanes
  
• Physicochemical Properties Of Alkanes, Alkenes And Cyclic Alkanes
  
• Alkyl Halides
  
• Definition And Nomenclature Of Alkyl Halides
  
• Physicochemical Properties Of Alkyl Halides
  
• Aromatic Compounds
  
• Definition And Nomenclature Of Aromatic Compounds
  
• Physicochemical Properties Of Aromatic Compounds
  
• Alcohols And Phenols
  
• Definition And Nomenclature Of Alcohols And Phenols
  
• Physicochemical Properties Of Alcohols And Phenols
  
• Ethers And Thioethers
  
• Definition And Nomenclature Of Ethers
  
• Physicochemical Properties Of Ethers
  
• Aldehydes And Ketones
  
• Definition And Nomenclature Of Aldehydes And Ketones
  
• Physicochemical Properties Of Aldehydes And Ketones
  
• Amines
  
• Definition And Nomenclature Of Amines
  
• Physicochemical Properties Of Amines
  
• Carboxylic Acids And Derivatives
  
• Definitions And Nomenclatures Of Carboxylic Acids And Derivatives
  
• Physicochemical Properties Of Carboxylic Acids And Derivatives
  
• Few Pharmaceutically Important Heterocyclic Ring Systems
  
• Five-Membered Unsaturated Heterocycles
  
• Six-Membered Unsaturated Heterocycles
  
• Fused-Ring Heterocycles
  
• Tricyclic, Tetracyclic And Bridged Ring Systems
  
• The Biomolecules
  
• Carbohydrates
  
• Classification Of Carbohydrates
  
• Other Important Carbohydrates And Derivatives
  
• Lipids
  
• Fatty Acids
  
• Glycerides (Acylglycerols)
  
• Phospholipids
  
• Eicosanoids
  
• Steroids
  
• Proteins
  
• Amino Acids
  
• Isoelectric Point Of Amino Acids
  
• Peptides And Proteins
  
• Primary, Secondary, Tertiary And Quaternary Protein Structures
  
• Nucleic Acids
  
• The Nucleotides And Nucleosides
  
• DNA Structure
  
• DNA Replication
  
• Rna Structure And Transcription
  
• Student Self-Study Guide
  
• Students Self-Assessment
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• References
  

Chapter 3 Acid-Base Chemistry And Salt Formation 

• Hardeep Singh Saluja And M O Faruk Khan
  
• Introduction
  
• Acid-Base Theories
  
• Arrhenius Concept
  
• Brønsted-Lowry Concept
  
• Lewis Concept
  
• Application Of Lewis And Brønsted-Lowry Definitions To Imidazole
  
• Acidic And Basic Functional Groups Occur In Drug Molecules
  
• Oxy Acids
  
• Thio Acids
  
• Amine Bases
  
• Aromatic Amines
  
• Acidic Amides (Azo Acids)
  
• ß-Diketone
  
• Acid-Base Strengths
  
• Acid-Conjugate Base And Base-Conjugate Acid
  
• Percent Ionization
  
• For Weak Acids (Ha Acids)
  
• For Weak Bases (Bh+ Acids)
  
• Electron Withdrawing Effect
  
• Electron Donating Effect
  
• Ph Partition Theory
  
• Salt Formation
  
• Definition Of Salts
  
• Organic Base Reacting With An Inorganic Acid
  
• Organic Acid Reacting With An Inorganic Base
  
• Organic Acid Reacting With An Organic Base
  
• Acidity Or Basicity Of Salts
  
• Case Studies
  
• Student Self-Study Guide
  
• Student Self-Assessment
  
• Part I: Multiple Choice Questions
  
• Part Ii: K-Type Question
  
• Part Iii: Matching Question
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• References
  

Chapter 4 Solubility And Lipid-Water Partition Coefficient 

• Hardeep Singh Saluja
  
• And M O Faruk Khan
  
• Solubility
  
• Factors Affecting Solubility
  
• Solvation
  
• Forces Involved In Solvation
  
• Polarity, Lipophilicity And Related Parameters
  
• Predicting Solubility Of Drugs Based On Functional Groups
  
• Lemke’S Empirical Method
  
• Cate’S Analytical Method
  
• Partition Coefficient
  
• Lipid-Water Partition Coefficient
  
• Application Of Partition Coefficient To Drugs
  
• Case Studies
  
• Student Self-Study Guide
  
• Student Self Assesment
  
• Part I - Multiple Choice Questions:
  
• Part III - K-Type Questions:
  
• Part III- Matching Questions:
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• References
  

Chapter 5 Isosteric And Spatial Considerations Of Drugs 

• Isosterism And Bioisosterism
  
• Isosterism In Drugs
  
• Spatial Consideration Of Drugs
  
• The Significance Of The Study Of Stereochemistry
  
• Stereochemical Definitions And Illustrations
  
• Cahn-Ingold-Prelog (CIP) Rules
  
• Cis-Trans Isomerism
  
• Student Self-Study Guide
  
• Students Self Assesment
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• References
  

Chapter 6 Fundamentals Of Drug Action 

• M O Faruk Khan And Taufiq-Rahman
  
• Historical Perspective
  
• Drug Receptors
  
• Mechanism Of Drug Action On Receptor Level
  
• Theories Of Drug Action
  
• Occupancy Theory
  
• Modification Of Occupancy Theory
  
• Rate Theory
  
• Induced-Fit Theory
  
• Macromolecular Perturbation Theory
  
• Occupation-Activation Theory Of “Two-State” Model
  
• Drug-Receptor Interactions
  
• The Interaction (Bond) Types
  
• Covalent Bonds
  
• Non-Covalent Bonds
  
• Students Self-Study Guide
  
• Students Self Assesment
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• References
  

Chapter 7 Drug Metabolism 

• Rahmat Talukder, Ashok Philip And M O Faruk Khan
  
• Introductory Concepts
  
• Roles Played By Drug Metabolism
  
• 1 Drug Inactivation Or Detoxification
  
• 2 Similar Activity
  
• 3 Different Activity
  
• 4 Intoxication
  
• 5 Activation
  
• Enzymes Involved In Drug Metabolism
  
• Oxidases
  
• Oxidoreductases
  
• Transferases
  
• Hydrolases
  
• Sites Of Drug Metabolism
  
• First-Pass Effect
  
• Enterohepatic Circulation
  
• Enzyme Induction & Inhibition
  
• Pathways Of Metabolism
  
• Phase I Metabolic Reactions
  
• Oxidation
  
• Aliphatic And Alicyclic Hydroxylations
  
• Alkene And Alkyne Hydroxylation
  
• Aromatic (Arene) Hydroxylation
  
• Oxidation Involving Carbon-Nitrogen Systems
  
• Oxidation Involving Carbon-Oxygen Systems: O-Dealkylation
  
• Oxidation Of Carbon-Sulfur Systems: S-Dealkylation, Desulfuration, And S-Oxidation
  
• Dehalogenation
  
• Oxidation Of Alcohols And Aldehydes
  
• Reductive Reactions
  
• Reduction Of Aldehydes And Ketones
  
• Nitro And Azo Reduction
  
• Azido Reduction
  
• Reduction Of Sulfur Containing Compounds
  
• Reductive Dehalogenation
  
• Hydrolytic Reactions
  
• Phase Ii Metabolic Reactions
  
• Glucuronic Acid Conjugation
  
• Sulfonate Conjugation
  
• Amino Acid Conjugation
  
• Glutathione Conjugation
  
• Acetyl Conjugation
  
• Fatty Acid And Cholesterol Conjugation
  
• Methyl Conjugation
  
• Stereochemistry And Drug Metabolism
  
• Itraconazol (Itz) Metabolism
  
• Etodolac Metabolism
  
• Etomidate Metabolism
  
• Warfarin Metabolism
  
• Propranolol Metabolism
  
• Pharmacologically Active Metabolites
  
• The Active Metabolites Of Tamoxifen And Thioridazine
  
• The Active Metabolites Of Metoprolol And Morphine
  
• Diazepam, Temazepam, And Oxazepam
  
• Active Metabolite Of Doxepine
  
• The Active Metabolites Of Atorvastatin
  
• Prodrugs, Soft Drugs And Antedrugs
  
• Introduction
  
• Common Functional Groups In Prodrugs
  
• Prodrugs With Increased Lipophilicity
  
• Prodrugs With Increased Hydrophilicity As Well As Parenteral Applicability
  
• Prodrugs With Improved Site-Specific Delivery
  
• Other Prodrugs
  
• The Soft Drugs And Antedrugs
  
• Factors Affecting Drug Metabolism
  
• Influence Of Age On Drug Metabolism
  
• Influence Of Sex On Drug Metabolism
  
• Genetic Polymorphism
  
• Effects Of Smoking On Drug Metabolism
  
• Effects Of Grapefruit Juice On Drug Metabolism
  
• Case Studies
  
• Student Self-Study Guide
  
• Student Self-Assessment
  
• Part I: Multiple Choice Questions
  
• Part II: K-Type Question Chose The Answer
  
• Part III: Matching Questions
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• References
  

Chapter 8 Biosynthetic Pathways Frequently Targeted By Pharmaceutical Intervention 

• Jason L Johnson M O Faruk Khan And Eicosanoid Biosynthesis
  
• Introduction
  
• Prostaglandins And Thromboxanes Biosynthesis: The “Cyclic” Pathway
  
• Leukotrienes And Lipoxins Biosynthesis: The “Linear” Pathway
  
• Epinephrine And Norepinephrine Biosynthesis
  
• Introduction
  
• Pathways
  
• Folic Acid Biosynthesis
  
• Introduction
  
• Pathways
  
• Steroid Biosynthesis
  
• Introduction
  
• Cholesterol Biosynthesis
  
• Adrenocorticoid Biosynthesis
  
• Sex Hormone Biosynthesis
  
• Nucleic Acid Biosynthesis
  
• Introduction
  
• Purine Biosynthesis
  
• Pyrimidine Biosynthesis
  
• Deoxyribonucleotide Biosynthesis
  
• Purine Catabolism
  
• Pyrimidine Catabolism
  
• Purine Salvage Pathway
  
• Pyrimidine Salvage Pathway
  
• Regulation Of Nucleotide Metabolism
  
• Student Self-Study Guide
  
• Consent For Publication
  
• Conflict Of Interest
  
• Acknowledgement
  
• Further Reading
  

Author

• M. O. Faruk Khan
  
• Ashok E. Philip