Front Cover

Front Matter

Copyright

Preface

Acknowledgements

Contents

Section I : Physicochemical Factors In Relation To Biological Activity Of Drugs

Introduction to Medicinal Chemistry

Processes of Drug Discovery

Discovery

Optimization

Development

Drug Discovery and Design-A Historical Outline

Modern Drug Discovery

Targets-New and Established

Screening and Designing

Nature as a Source of Drug Compounds

Plant-Derived Bioactive Materials

Microbial Species with Bioactive Metabolites

Marine Invertebrates as a Source of Bioactive Compounds

Chemical Diversity of Natural Products

Methodologies in Natural Product Drug Discovery

Identification of Biologically Active Material

Structural Elucidation

Drug Designing

Rational Drug Design

Computer-Assisted Drug Design

Chapter 1 - Physicochemical Properties

Introduction

Chapter 2 - Ferguson Principle

Introduction

Chapter 3 - Hydrogen Bonding

Introduction

Classification

Chapter 4 - Ionization and pKa Value

Introduction

pKa Value

Drug Exerting Action as Undissociated Molecules

Drug Exerting Action as Ionized Molecules

Chapter 5 - Redox Potential

Introduction

Chapter 6 - Surface Tension

Introduction

Classification

Applications

Chapter 7 - Complexation

Introduction

Chapter 8 - Steric Features of Drugs

Introduction

Conformational Isomers

Optical Isomers

Enantiomers

Diastereomers

Reasons Behind Varying Activity of Optical Isomers

Binding of Enantiomers to Receptors

Chapter 9 - Bioisosterism

Introduction

Classification

Section II : Drug Design

Chapter 1 - Concepts of Drug Design

Introduction

Design of Analogues and Prodrugs

Design of Lead and Lead Discovery

Approaches to Lead Discovery

Random Screening

Nonrandom Screening

Pharmacokinetic Studies

Pharmacodynamic Studies

Drug Design Through Disjunction

Drug Design Through Conjunction

Molecular Hybridization in Drug Design

Rational Approach to Drug Design

Chapter 2 - Receptors

Introduction

Types of Receptors

Theories of Receptors

Occupation Theory

Rate Theory

Induced Fit Theory

Macromolecular Perturbation Theory

Activation-Aggregation Theory

Forces Involved in Drug Receptors Interaction

Covalent Bonding

Dipole-Dipole and Ion-Dipole Interactions

Hydrogen Bonding

Electrostatic Bonding

Charge Transfer Complex

Hydrophobic Forces

van der Waal's or London Dispersion Forces

Factors Affecting the Drug-Receptor Interaction

Chapter 3 - Computer-Aided Drug Design

Introduction

Bioinformatics Hub

Advantages of CADD

Chapter 4 - Structure-Activity Relationship and Quantitative Structure-Activity Relationship

Introduction

Historical Development of QSAR

Hansch Analysis

Free-Wilson Analysis

Mixed Approach

Advantages of QSAR

Disadvantages of QSAR

Basic Requirements for QSAR Analysis

Steps Involved in QSAR Studies

Statistical Methods Used in QSAR Analysis

Regression Methods

Partial Least Square (PLS)

Genetic Function Approximation (GFA)

Genetic Partial Least Squares (G/PLSs)

Principal Component Analysis (PCA)

Statistical Measures Commonly Used in Regression Analysis

Model Development Procedures

Classical or 2D QSAR Analysis

3D-QSAR Analysis

Comparative Molecular Field Analysis (CoMFA)

Comparative Molecular Similarity Indices Analysis (CoMSIA)

Chapter 5 - Combinatorial Chemistry

Introduction

Principles of Combinatorial Chemistry

Combinatorial Compound Libraries

Combinatorial Synthesis on Solid Phase

Advantages and Disadvantages of Solid Support Reagents

Resins for SPS

Chapter 6 - Pro-Drugs

Introduction

Ideal Properties

Classification of Pro-Drug

Applications of Pro-Drug

Improvement of Taste

Improvement of Odour

Enhancement of Bio-Availability (Lipophilicity)

Improvement of Stability and Solubility

Decreased Toxicity and Adverse Reactions

Site-Specific Drug Delivery

Increased duration of action

Bio-Precursor Prodrug

Section III : Drugs Acting Oncentral Nervoussystem

Chapter 1 - Central Nervous System

Introduction

Amino Acids

Adrenergic Pathway in CNS

Functional Aspects of Dopamine

Functional Aspects of 5-HT

Cholinergic Transmission in CNS

Other Neurotransmitters and Functions in CNS

Chapter 2 - Sedatives and Hypnotics

Introduction

Treatment of Anxiety States

Treatment of Sleep Problems

Other Therapeutic Uses

Molecular Basis of Inhibitory Neurotransmitters

Classification

Synthesis and Drug Profile

SAR of Barbiturates

SAR of Benzodiazepines

Chapter 3 - General Anaesthetics

Introduction

Types of General Anaesthetics

Stages of Anaesthesia

Classification

Synthesis and Drug Profile

Chapter 4 - Local Anaesthetics

Introduction

Classification

Synthesis and Drug Profile

Sar of Benzoic Acid Derivatives

SAR of Anilides

Chapter 5 - Tranquillizers

Introduction

General Mode of Action

Classification

-->Synthesis and drug profile

SAR of Phenothiazines

SAR of Butyrophenones

Chapter 6 - Antidepressants

Introduction

Uses

Classification

Synthesis and drug profile

SAR of Dibenzazepines

-->SAR of Dibenzo Cycloheptane Derivatives

Chapter 7 - CNS Stimulants

Introduction

Classification

Synthesis and Drug Profile

Xanthine Derivatives

Chapter 8 - Narcotic Analgesics

Introduction

Opioid Analgesics

General Mode of Action

Therapeutic Uses

Classification

Synthesis and Drug Profile

SAR of morphine

SAR of Meperidine Analogues

SAR of Diphenyl Heptanone (Methadone Series)

SAR of Benzomorphan Derivatives (Benzazocines)

Narcotic Antagonists

Classification

Chapter 9 - Anticonvulsants

Introduction

Classification

Pharmalocogical Classification

Synthesis and Drug Profile

SAR of Barbiturates

SAR of Hydantoins

SAR of Oxazolidinediones

SAR of Succinimides

SAR of Phenacemide

SAR of Sodium Valproate

Chapter 10 - Antiparkinsonism Agents

Introduction

Classification

Synthesis and Drug Profile

Chapter 11 - Skeletal Muscle Relaxants

Introduction

Classification

Synthesis and Drug Profile

Chapter 12 - Alzheimers Disease

Introduction

Pathogenesis

Treatment

Acetylcholinesterase Inhibitors

NMDA Antagonists

Tacrine

Section IV : Drugs Acting Onautonomic Nervoussystem

Chapter 1 - Autonomic Nervous System

Introduction

Sympathetic System

Neurotransmission

Regulation of Catecholamines

Adrenergic Receptors

-Receptors

-Receptors

Parasympathetic System

Neurotransmission

Regulation of Ach

Cholinergic Receptors

Muscarinic Receptors

Nicotinic Receptors

Chapter 2 - Adrenergic Drugs

Introduction

Physiological Basis of Adrenergic Receptor Function

Mechanism of Action of Sympathomimetics

1 Adrenergic Receptor Action

2 Adrenergic Receptor Action

1 Adrenergic Receptor Action

2 Adrenergic Receptor Action

General Classification of Adrenerigic Agonists

Classifications Based on Therapeutic Uses

Classification Based on Chemical Structures

Synthesis and Drug Profile

Structural-Activity Relationship

Chapter 3 - Cholinergic Drugs

Introduction

Spectrum of Cholinomimetic Drugs

Direct-acting Cholinoceptor Stimulants

Mechanism of Action of Directly Acting Cholinergic Drugs

Indirect Acting Cholinomimetic Drugs

Mechanism of Action of Indirectly Acting Cholinergic Drugs (Anticholinesterase Agents)

Classification

Synthesis and Drug Profile

Structure Activity Relationship

Chapter 4 - Adrenergic Blockers

Introduction

Physiological Basis of Adrenergic Receptor Antagonists

Mechanism of Action of -Adrenergic Blockers

Mechanism of Action of -Adrenergic Receptor Blockers

Classification

Synthesis and Drug Profile

Structure-Activity Relationship

Chapter 5 - Anticholinergic Drugs

Introduction

Difference Between the Quaternary and the Tertiary Antimuscarinics

Quaternary Amines

Tertiary Amines

Therapeutic Uses

Classification

Synthesis and Drug Profile

SAR Solanaceous Alkaloids (Atropine Analogues)

SAR of Muscarinic Antagonists

Section V : Drugs Acting Oncardiovascularsystem

Chapter 1 - Cardiovascular System

Introduction

Aetiology of Hypertension

Normal Regulation of Blood Pressure

Chapter 2 - Antihypertensive Drugs

Introduction

Hypertension

Primary Hypertension

Secondary Hypertension

Classification

Synthesis and Drug Profile

Chapter 3 - Antiarrhythmic Drugs

Introduction

Classification

Synthesis and Drug Profile

Chapter 4 - Antihyperlipidaemic Agents

Introduction

Classification

Synthesis and Drug Profile

Chapter 5 - Antianginals

Introduction

Principles of Therapy for Angina

Classification

Synthesis and Drug Profile

Sar of Dihydropyridines

Second-Generation Alkyl Amine Type Calcium Channel Blockers

Section VI : Drugs Acting Onurinary System

Chapter 1 - Urinary System

Introduction

Functions of Renal System

Principle of Glomerular Filtration

Principle of Tubular Reabsorption and Secretion

Chapter 2 - Diuretics

Introduction

Classification

Synthesis and Drug Profile

SAR of Thiazide Diruretics

SAR of CAse Inhibitiors

SAR of Loop Diuretics

Properties

Index

A

B

C

D

E

F

G

H

I

K

L

M

N

O

P

Q

R

S

T

U

V

W

X

Z