Fundamentals of Medicinal Chemistry and Drug Metabolism

 
 
Medicinal Chemistry for Pharmacy Students (Verlag)
  • 1. Auflage
  • |
  • erschienen am 1. Juni 2018
  • |
  • 350 Seiten
 
E-Book | ePUB mit Adobe DRM | Systemvoraussetzungen
978-1-68108-687-3 (ISBN)
 

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 chemical basis of drug action. This first volume of the series is

  • Englisch
  • Sharjah
  • |
  • Vereinigte Arabische Emirate
PublishDrive
  • 8,36 MB
978-1-68108-687-3 (9781681086873)
weitere Ausgaben werden ermittelt
  • Intro
  • Introduction
  • M. O. Faruk Khan1,* and Ashok Philip2
  • BRIEF HISTORY AND ROLE OF PHARMACISTS
  • BRIEF HISTORY OF MEDICINAL CHEMISTRY
  • DEFINITION OF MEDICINAL CHEMISTRY
  • MEDICINAL CHEMISTRY IN PHARMACY EDUCATION
  • An Abridged Medicinal Chemistry Vocabulary [15]
  • Medicinal Chemistry in Drug Discovery and Development
  • SCOPE OF THIS BOOK SERIES
  • CONSENT FOR PUBLICATION
  • CONFLICT OF INTEREST
  • ACKNOWLEDGEMENT
  • REFERENCES
  • Review of Bioorganic Chemistry
  • M. O. Faruk Khan1,* and Ashim Malhotra2
  • 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 (Fig. 9)
  • 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 (Fig. 22)
  • 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
  • Acid-base Chemistry and Salt Formation
  • Hardeep Sing Saluja1 and M. O. Faruk Khan2,*
  • 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
  • Solubility and Lipid-Water Partition Coefficient
  • Hardeep Sing Saluja1 and M. O. Faruk Khan2,*
  • 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 [7]
  • Cate's Analytical Method [7]
  • 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 II - K-Type Questions:
  • Part III - Matching Questions:
  • CONSENT FOR PUBLICATION
  • CONFLICT OF INTEREST
  • ACKNOWLEDGEMENT
  • REFERENCES
  • Isosteric and Spatial Considerations of Drugs
  • M. O. Faruk Khan1,* and Timothy J. Hubin2
  • 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 [9]
  • Cis-Trans Isomerism
  • STUDENT SELF-STUDY GUIDE
  • STUDENTS SELF ASSESMENT
  • CONSENT FOR PUBLICATION
  • CONFLICT OF INTEREST
  • ACKNOWLEDGEMENT
  • REFERENCES
  • Fundamentals of Drug Action
  • M. O. Faruk Khan1,* and Taufiq Rahman2
  • 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
  • Drug Metabolism
  • Rahmat Talukder1, Ashok Philip2 and M. O. Faruk Khan3,*
  • 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
  • Biosynthetic Pathways Frequently Targeted by Pharmaceutical Intervention
  • Jason L. Johnson1 and M. O. Faruk Khan2,*
  • 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
  • Subject Index

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