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Файл:Ординатура / Хирургия / Библиотека им академика М.И. Перельмана / Книга_5726_Библиотеки_им_академика_М_И_Перельмана.pdf
A TEXTBOOK OF
Medicinal Chemistry
A TEXTBOOK OF
Medicinal Chemistry
Munendra Mohan Varshney
Assistant Professor
Department of Pharmaceutical Sciences
Raj Kumar Goel Institute of Technology, Ghaziabad
Asif Husain
Assistant Professor
Department of Pharmaceutical Chemistry
Jamia Hamdard University, New Delhi
©Copyright 2020 I.K. International Pvt. Ltd., New Delhi-110002.
This book may not be duplicated in any way without the express written consent of the publisher,
except in the form of brief excerpts or quotations for the purposes of review. The information
contained herein is for the personal use of the reader and may not be incorporated in any commercial
programs, other books, databases, or any kind of software without written consent of the publisher.
Making copies of this book or any portion for any purpose other than your own is a violation of
copyright laws.
Limits of Liability/disclaimer of Warranty: The author and publisher have used their best efforts in
preparing this book. The author make no representation or warranties with respect to the accuracy or
completeness of the contents of this book, and specifically disclaim any implied warranties of
merchantability or fitness of any particular purpose. There are no warranties which extend beyond the
descriptions contained in this paragraph. No warranty may be created or extended by sales
representatives or written sales materials. The accuracy and completeness of the information provided
herein and the opinions stated herein are not guaranteed or warranted to produce any particulars
results, and the advice and strategies contained herein may not be suitable for every individual.
Neither Dreamtech Press nor author shall be liable for any loss of profit or any other commercial
damages, including but not limited to special, incidental, consequential, or other damages.
Trademarks: All brand names and product names used in this book are trademarks, registered
trademarks, or trade names of their respective holders. Dreamtech Press is not associated with any
product or vendor mentioned in this book.
ISBN: 978-93-89633-59-7
EISBN: 978-93-89976-93-9
Edition: 2020
Preface
Medicinal chemistry plays a vital role in pharmaceutical research to synthesize and analyse novel
bioactive medicinal compounds. The actual phase of identification and optimum bioactive position
on the basic skeleton of lead molecule is the important aspect for biological activity and for further
research.
The advancement of recent developments in medicinal chemistry has been taking place rapidly.
We have tried to enrich with latest developments in the book. This book is meant for undergraduate
students of Pharmacy and those who offer medicinal chemistry as part of course curriculum. This
book emphasizes the fundamentals of medicinal chemistry aspects, various classifications, drug
synthesis, drug action and their pharmacological uses with recent developments of various classes
of drug action and their pharmacological uses with recent developments of various classes of
drugs. Thus, it would be beneficial to the readers to extend knowledge in respect of several known
classes of drug molecules.
Suggestions and criticism for further improvement are welcome and we are responsible for all
kinds of errors that might have crept in and we will be grateful if the readers bring them to our
attention.
Munendra Mohan Varshney
Asif Husain
Contents
Preface v
1. Physical Chemical Factors and Biological Properties 1
1.1 Introduction 1
1.2 Types of Drug Action Theories 1
1.2.1 The Ferguson Principle 1
1.2.2 Structure and Activity 2
1.2.3 Relationship between Molecular Structure and Biological Action 3
1.3 Physicochemical Parameters and Pharmacological Activity 3
1.3.1 Introduction 3
1.3.2 Solubility Parameters 3
1.3.3 Steric Parameters 7
1.4 Stereochemistry Consideration 7
1.4.1 Chirality 7
1.4.2 Stereochemistry and Drug Action 8
1.4.3 Isomers Types 9
1.5 Isosterism and Bioisosterism 11
1.5.1 Pharmacophore or Lead 11
1.5.2 Isosteres 11
1.5.3 Bioisosteres 11
1.6 Drug-Receptor Interaction 13
1.6.1 Receptor 13
1.6.2 Requirement for Agonist Activity 15
1.6.3 Receptor Families 15
1.6.4 Role of Chemical Bonding 15
1.6.5 Types of Receptors 16
1.7 Prodrugs 17
1.7.1 Introduction 17
1.7.2 Concept of Prodrug 18
1.7.3 Prodrugs are Designed for the Following Purposes 18
1.7.4 Classification of Prodrugs 18
Exercise 21
viii Contents
2. Autonomic Nervous System Cholinergic Drugs and Adrenergic Agents 23
Autonomic Nervous System 23
2.1 Introduction 23
2.2 Cholinergic Drugs 24
2.2.1 Definition 24
2.2.2 Cholinergic Receptors 25
2.2.3 Biosynthesis of Ach 25
2.2.4 Classification 26
2.2.5. Action of Cholinesterase Inhibitors 30
2.2.6 Structural Activity Relationship (SAR) of Musarinic Agonist/
Cholinomimetics 30
2.2.7 Cholinomimetic Agents 31
2.2.8 Anticholinergic/Cholinergic Blocking Agents/Parasympatholytics/
Antispasmodics Agents/Muscarinic Receptors Antagonist 33
2.2.9 Classification of Anticholinergic Agents 34
2.2.10 Structural Activity Relationship (SAR) of Anticholinergic Agent 36
2.2.11 Anticholinergic Agent 36
2.2.12 Newer Drug 39
2.3 Adrenergic Agents 39
2.3.1 Introduction 39
2.3.2 Mechanism of Action 40
2.3.3 Biosynthesis of Catecholamines 40
2.3.4 Pharmacological Action 40
2.3.5 Adrenergic 41
2.3.6 Classification 42
2.3.7 SAR of Phenylethanolamine Derivatives/Direct Acting Agonist 45
2.3.8 SAR of Indirect Acting Agonist/Arylethylamine Derivatives 47
2.3.9 Adrenergic Agents 47
2.3.10 Newer Drugs 51
Exercise 52
3. General Anaesthetics 53
3.1 Introduction 53
3.2 Ideal Characteristics of General Anaesthetics 53
3.3 Important Physiological Properties Responsible for Entry of
Compounds into Brain 54
3.4 Concepts of Mechanism of Anaesthesia 54
3.5 Minimum Alveolar Concentration (MAC) 54
3.6 Stages of Anaesthesia 55
3.7 Classification of General Anaesthesia 55
3.8 Receptors Involved in the Mechanism 58
3.9 Stereochemistry of Volatile Anaesthetics 58
3.10 Toxicity of Fluorinated General Anaesthetics 58