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Fundamentals of Medicinal Chemistry and Drug Metabolism

  • ID: 4582205
  • Book
  • Bentham Science Publishers Ltd
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The primary objective of this 4-volume book series is to educate PharmD students on the subject of medicinal chemistry. The book set serves as a reference guide to pharmacists on aspects of the chemical basis of drug action. This first volume of the series is comprised of 8 chapters focusing on basic background information about medicinal chemistry. It takes a succinct and conceptual approach to introducing important fundamental concepts required for a clear understanding of various facets of pharmacotherapeutic agents, drug metabolism and important biosynthetic pathways that are relevant to drug action. Notable topics covered in this first volume include the scope and importance of medicinal chemistry in pharmacy education, a comprehensive discussion of the organic functional groups present in drugs, and information about four major types of biomolecules (proteins, carbohydrates, lipids, nucleic acids) and key heterocyclic ring systems.

The concepts of acid-base chemistry and salt formation, and their applications to the drug action and design follow thereafter. These include concepts of solubility and lipid-water partition coefficient (LWPC), isosterism, stereochemical properties, mechanisms of drug action, drug receptor interactions critical for pharmacological responses of drugs, and much more. Students and teachers will be able to integrate the knowledge presented in the book and apply medicinal chemistry concepts to understand the pharmacodynamics and pharmacokinetics of therapeutic agents in the body.

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