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Copyright © 2007, 2005, 2000, 1993 NewAge International (P) Ltd., Publishers
Published by New Age International (P) Ltd., ...
DEDICATION
This Fourth Revised and Expanded Edition of Medicinal Chemistry is
dedicated to :
(Late) Professor Chandrashekh...
From Reviews of the Previous Editions
“It deals exhaustively with the major clinically useful drugs of various classes and...
PREFACE TO THE FOURTH EDITION
The success in succession of Medicinal Chemistry has been a phenomenal achievement since
the...
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PREFACE TO THE FIRST EDITION
This book, ‘Medicinal Chemistry’ has two objectives in view. The first objective is to attrac...
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(xi)
CONTENTS
Preface to the Fourth Edition (vii)
Preface to the First Edition (ix)
CHAPTER 1: Drug Design—A Rational Appr...
(xii)
2.4. Thermodynamic Activity 24
2.5. Meyer-Overton and Meyer-Hemmi Theory 24
2.6. Ferguson’s Theory 25
2.7. Van der W...
(xiii)
CHAPTER 3: Molecular Modeling and Drug Design 59
1. Introduction 60
2. Methodologies : Molecular Modeling 61
2.1. M...
(xiv)
5. Predictive ADME 90
6. Reverse Designing 92
6.1. High Throughput Screening 92
6.2. Combinatorial Chemistry 92
7. C...
(xv)
4. Benzoic Acid and Aniline Analogues with Potential Local
Anaesthetic Profile 161
5. Mode of Action of Some Selected...
(xvi)
CHAPTER 9: Central Nervous System Stimulants 253
1. Introduction 254
2. Classification 255
2.1. Xanthine Derivatives...
(xvii)
4.4. 4-Phenylpiperidine Analogues 322
4.5. Phenylpropylamine Analogues 327
4.6. Miscellaneous Analogues 330
5. Narc...
(xviii)
4. Beta Adrenergic Receptor Stimulants 386
4.1. Mechanism of Action 387
5. Adrenergic Receptor Blocking Agents 388...
(xix)
2.2.4. ‘Loop’ and ‘High-Ceiling’ Diuretics 467
2.2.5. Aldosterone Inhibitors 471
2.2.6. Purine or Xanthine Diuretics...
(xx)
2.6. Miscellaneous Anti-Inflammatory Drugs 538
2.6.1. Antimalarial Agents 538
2.6.2. Uricosuric Agents 538
2.7. Salic...
(xxi)
2.5. Sulphonamide Related Compounds 604
2.5.1. Mechanism of Action 606
3. Ionizaton of Sulphonamides 607
4. Sulphona...
(xxii)
3. Oral Hypoglycemic Agents 672
3.1. Sulfonylureas 672
3.1.1. First-Generation Sulfonylureas 673
3.1.2. Second-Gene...
(xxiii)
4. Aminoglycoside Antibiotics 763
5. Chloramphenicol 767
5.1. Structure of Chloramphenicol 767
5.2. Synthesis of C...
(xxiv)
2.3. Antibiotics 817
2.3.1. Mechanism of Action 819
2.4. Plant Products 819
2.4.1. Imides and Amides 820
2.4.2. Ter...
(xxv)
2.2. Substances that Interfere with Viral Nucleic Acid Replication 857
2.2.1 Mechanism of Action 859
2.3. Substances...
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1
Drug Design—A Rational Approach
1. INTRODUCTION
In the past few decades there has been a hiatus in the momentum of research and discovery of
‘novel medici...
DRUG DESIGN—A RATIONAL APPROACH 3
CHAPTER1
In the recent past, another terminology ‘prodrugs’ has been introduced to make ...
4 MEDICINAL CHEMISTRY
Ehrhardt suggested a general formula relevant to the analgesic activity in 1949 as stated below :
O
...
DRUG DESIGN—A RATIONAL APPROACH 5
CHAPTER1
Quite recently phenacetine has been withdrawn completely because of its toxic a...
6 MEDICINAL CHEMISTRY
4. FACTORS GOVERNING DRUG-DESIGN
A few cardinal factors governing the efficacy towards the evaluatio...
DRUG DESIGN—A RATIONAL APPROACH 7
CHAPTER1
5.1. Quantum Mechanical Approach
Quantum mechanics (or wave mechanics) is compo...
8 MEDICINAL CHEMISTRY
• To modify specificity of action
• To improve duration of action
• To reduce toxicity
• To effect e...
DRUG DESIGN—A RATIONAL APPROACH 9
CHAPTER1
Example :
The extensive study on the estrogenic activity of oestradiol via drug...
10 MEDICINAL CHEMISTRY
From the above the following three observations may be made. They include :
(i) Various steps in de...
DRUG DESIGN—A RATIONAL APPROACH 11
CHAPTER1
(where Sv1 = steric factor 1 ; Sv2 = steric factor 2 ; Sv3 = steric factor 3 ;...
12 MEDICINAL CHEMISTRY
*Sneader WJ, ‘Drug Discovery : The Evolution of Modern Medicines,’ John Wiley, Chichester, UK,
1997...
DRUG DESIGN—A RATIONAL APPROACH 13
CHAPTER1
The various phases of transformations in ‘ethical pharmaceutical industry’ bet...
14 MEDICINAL CHEMISTRY
7.3. Research and Development Strategies
It has been proved beyond any reasonable doubt that the ‘r...
DRUG DESIGN—A RATIONAL APPROACH 15
CHAPTER1
A few typical examples wherein the hyberdisation was accomplished commencing f...
16 MEDICINAL CHEMISTRY
9. RIGIDITY AND FLEXIBILITY Vs DRUG DESIGN
It has been observed beyond any reasonable doubt whatsoe...
DRUG DESIGN—A RATIONAL APPROACH 17
CHAPTER1
Interestingly, either of the two structural analogues (A) and (B) can be furth...
18 MEDICINAL CHEMISTRY
9.2. Increased Flexibility
The problems encountered invariably with less flexible, rigid and compac...
DRUG DESIGN—A RATIONAL APPROACH 19
CHAPTER1
An effective drug design from a biologically active prototype, whether approac...
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2
Physical-Chemical Factors
and Biological Activities
+D=FJAH
1. INTRODUCTION
The quest for knowledge to establish how the drugs act in a living system has been a thought-
prov...
PHYSICAL-CHEMICAL FACTORS AND BIOLOGICAL ACTIVITIES 23
CHAPTER2
vis-a-vis their affect upon biological activities. General...
24 MEDICINAL CHEMISTRY
The apparent effect of structure on biological activity may be observed in the following examples
w...
PHYSICAL-CHEMICAL FACTORS AND BIOLOGICAL ACTIVITIES 25
CHAPTER2
S.No. Compounds Partition coefficient Required conc. to Ca...
26 MEDICINAL CHEMISTRY
R = Gas constant,
a = Constant for attractive forces between molecules and
b = Constant for volume ...
PHYSICAL-CHEMICAL FACTORS AND BIOLOGICAL ACTIVITIES 27
CHAPTER2
Fig. 2.1. Interaction between ‘Saturation-Line S’ and ‘Log...
28 MEDICINAL CHEMISTRY
characteristics. In fact, a plethora of methodologies have been tried and tested to ascertain the s...
PHYSICAL-CHEMICAL FACTORS AND BIOLOGICAL ACTIVITIES 29
CHAPTER2
the overall equilibrium shall influence and shift more to ...
30 MEDICINAL CHEMISTRY
Fig. 2.4(a) Electronic Influence on R Caused due to Resonance
and Inductive Effects of p-nitro Func...
PHYSICAL-CHEMICAL FACTORS AND BIOLOGICAL ACTIVITIES 31
CHAPTER2
Explanations : For Resonance Structures of Aniline [Fig. 2...
32 MEDICINAL CHEMISTRY
2.9.3. Verloop Steric Parameter
The unique revelation and wisdom of a latest computer researched pr...
PHYSICAL-CHEMICAL FACTORS AND BIOLOGICAL ACTIVITIES 33
CHAPTER2
2.10. Hansch Equation
Integrating various factors, namely ...
34 MEDICINAL CHEMISTRY
σ = Hammett substitution constant
a, b, d = Constants of the system (which are determined by comput...
PHYSICAL-CHEMICAL FACTORS AND BIOLOGICAL ACTIVITIES 35
CHAPTER2
(2) The corresponding constant is low (0.14) which reflect...
36 MEDICINAL CHEMISTRY
(2) From the above Craig plot one may obviously identify the substituents that are particu-
larly r...
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medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
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medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
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medicinal-chemistry By Ashutosh kar
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medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
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medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
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medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
medicinal-chemistry By Ashutosh kar
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medicinal-chemistry By Ashutosh kar

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medicinal chemistry by well known prof. Ashutosh kar.
contains various covered like drugs,steriods,analgesics,antibiotics,antimalarials,antimicrobial drugs,adrenocortical steroids,new drugs for newer diseases,antineoplastic agents,anthelmintics,sulphanomids,autonomic drugs,narcotic analgesics,central nervous system stimulants,anticonvulsants,muscle relaxants,sedatives and hypnotics,Molecular modelling and drug design etc



Hope u like it:-)

Published in: Education, Technology