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A Textbook of Pharmaceutical
Chemistry
Dr. Rahul Gajanan Ingle
Principal,
Dr. Rajendra Gode College of Pharmacy,
Amravati.
Dr. Ravindra Dattatraya Yeole
M.Pharm., Ph.D.,
Vice-President, Drug Discovery,
Wockhardt Research Centre,
Aurangabad.
Dr. Rajendra Panditrao Marathe
M.Pharm., Ph.D.,
Professor and I/c Principal,
Government College of Pharmacy,
Ratnagiri.
ISO 9001:2015 CERTIFIED
© Authors
No part of this publication may be reproduced, stored in a retrieval system, or transmitted in any form or by any
means, electronic, mechanical, photocopying, recording and/or otherwise without the prior written permission of the
publisher.
First Edition : 2022
Published by : Mrs. Meena Pandey for Himalaya Publishing House Pvt. Ltd.,
“Ramdoot”, Dr. Bhalerao Marg, Girgaon, Mumbai - 400 004.
Phone: 022-23860170, 23863863; Fax: 022-23877178
E-mail: himpub@bharatmail.co.in; Website: www.himpub.com
Branch Offices :
New Delhi : “Pooja Apartments”, 4-B, Murari Lal Street, Ansari Road, Darya Ganj,
New Delhi - 110 002. Phone: 011-23270392, 23278631; Fax: 011-23256286
Nagpur : Kundanlal Chandak Industrial Estate, Ghat Road, Nagpur - 440 018.
Phone: 0712-2721215, 2721216
Bengaluru : Plot No. 91-33, 2nd Main Road, Seshadripuram, Behind Nataraja Theatre,
Bengaluru - 560 020. Phone: 080-41138821; Mobile: 09379847017, 09379847005
Hyderabad : No. 3-4-184, Lingampally, Besides Raghavendra Swamy Matham, Kachiguda,
Hyderabad - 500 027. Phone: 040-27560041, 27550139
Chennai : No. 34/44, Motilal Street, T. Nagar, Chennai - 600 017. Mobile: 09380460419
Pune : “Laksha” Apartment, First Floor, No. 527, Mehunpura, Shaniwarpeth
(Near Prabhat Theatre), Pune - 411 030. Phone: 020-24496323, 24496333;
Mobile: 09370579333
Cuttack : Plot No. 5F-755/4, Sector-9, CDA Market Nagar, Cuttack - 753 014, Odisha.
Mobile.: 09338746007
Kolkata : 3, S.M. Bose Road, Near Gate No. 5, Agarpara Railway Station,
North 24 Parganas, West Bengal - 700 109. Mobile: 09674536325
DTP by : Priyanka M.
Printed at : Kohli Printo Fast, Delhi. On behalf of HPH.
Foreword
New drug product reaches the patient at least after a decade of intense research and approval
from regulatory agencies. Actual drug discovery begins at a laboratory bench of pharmaceutical or
medicinal chemists. Therefore, knowing this subject is essential for every pharmacy student whether
he or she works as a retail pharmacist, as a hospital pharmacist, at a drug manufacturing company, or
in research.
The pharmacist should remain updated about all the information of the existing drugs concerning
to their synthesis, mechanism of action, type of formulation, storage, side-effects, interactions, and
use. It is not possible to include this vast information of all the commercially available drugs, but the
authors have included all the important drugs of each therapeutic class as per the syllabus. Authors
have made this book student-centric by describing each scientific terminology.
This textbook will serve as a valuable source of information for students, teachers, and all the
readers in the field of pharmacy. This book should create instinct in the minds of students to go for
higher studies and especially in research.
Prof. Shrikant Kalikar
Ex-HOD
Dept. of Pharmacy, Government Polytechnic, Amravati.
Preface
Amongst the subjects studied during either diploma or degree pharmacy course, the
Pharmaceutical Chemistry or Medicinal Chemistry stands different; this is because it deals with the
actual drug (medicine) molecules which are invented, undergo clinical trials, manufactured,
formulated, get approval from regulatory authorities, prescribed and used by the end consumer, that is
patient, for either preventive or cure of the disorder or disease. These drug molecules act upon the
receptors, pathogens at a molecular level and exhibit required pharmacodynamic action.
Pharmacy Council of India released the new education regulations in 2020 for the “Diploma in
Pharmacy” course wherein the new syllabus of the “Pharmaceutical Chemistry” has been designed to
make aware the student about chemistry and uses of drug substance, its storage conditions along with
knowledge of the impurities, and way of testing them.
The authors have worked for almost one-and-a-half years to write the first edition of
“Pharmaceutical Chemistry”. The authors have used their knowledge and experience; have referred to
hundreds of books, journals, and pharmacopoeias to gather the information. This book covers whole
syllabus, and is written in a very simple and easy to understand language for the students. This book
has been divided in sections such as chapters on general topics, analysis, and nomenclature of organic
systems, inorganic and organic pharmaceuticals.
This book shall be useful not only to students but also to subject teachers.
There are numerous colleagues, friends, associates and family members to thank for their
encouragement and timely assistance. We are indebted to our publisher “Himalaya Publishing House
Pvt. Ltd.” for their guidance, corrections in manuscript, cover design and making this book available
to you.
The authors are happy to receive any comments and views, which will help us to improve upon.
Authors
Contents
Introduction to Pharmaceutical Chemistry 1 – 2
1. General Information 3 – 7
2. Limit Tests 8 – 14
3. Volumetric Analysis 15 – 19
4. Titrations 20 – 42
5. Nomenclature of Organic Chemical Systems 43 – 49
6. Inorganic Pharmaceuticals 50 – 58
7. Drugs Acting on Central Nervous System (CNS) 59 – 80
8. Drugs Acting on Autonomic Nervous System (ANS) 81 – 111
9. Drugs Acting on Cardiovascular System (CVS) 112 – 129
10. Diuretics 130 – 134
11. Hypoglycemic Agents 135 – 139
12. Non-steroidal Anti-inflammatory Agents 140 – 148
13. Anti-infective Agents 149 – 182
14. Antibiotics 183 – 202
15. Anti-neoplastic Agents 203 – 216
Bibliography 217 – 218
Question Bank 219 – 225
General Information
1
Introduction to
Pharmaceutical
Chemistry
The pharmaceutical industry is a knowledge-based industry, wherein the main thrust is
innovation, development, and quality production of drugs. Currently the entire pharmaceutical
industry is facing tough challenges in innovation and productivity. The major hurdles are the
increasing cost of research and development, tougher rules by the regulatory bodies, and thus
resulting in the declined number of new drug approvals.
Medicinal Chemistry and Pharmaceutical Chemistry are disciplines at the intersection of
chemistry, especially synthetic organic chemistry, pharmacology, and various other biological
specialties, where they are involved with the design, chemical synthesis, and development for the
commercialization of the new drugs.
Pharmaceutical Chemistry is the chemistry of substances useful as medicines.
Pharmaceutical Chemistry is an interdisciplinary science that is concerned with the discovery,
isolation, determination of structure, synthesis, analysis, and development of compounds that may
be useful as medicines. It also involves the study of metabolism and mechanism of action of
biologically active compounds at the molecular level and the relationship between the structures
and biological activity. Pharmaceutical Chemistry is also treated under the term medicinal
chemistry.
The disciple of Pharmaceutical Chemistry is committed to the discovery and development of
new drugs to improve the quality of life of animals and human beings.
According to Berger, “Medicinal Chemistry tries to be based on the ever-increasing hope
that biochemical rationale for drug discovery may be found”.
The first use of synthetic molecules in medicine was of anesthesia in the first half of the 19
th
century. Phenacetin was the first drug to be designed for biochemical transformations.
Ehrlich concluded that drug tolerance was developed when the drug get saturated or not
absorbed by the parasite. His ideas were supported by experimental facts.
The pharmaceutical agents mainly consist of inorganic compounds, organic compounds,
radiopharmaceuticals, and biotechnology products. Inorganic compounds which are important in
2
A Textbook of Pharmaceutical
Chemistry
therapy are trace elements in nutritional therapy, antacids, and radiopharmaceuticals, but organic
compounds with potent biological activities are dominant. The development of organic
compounds has been grown beyond traditional synthetic methods, for example biotechnology.
Biotechnology uses cell culture to synthesize new compounds. The pharmacist now dispenses
modified human insulin that provides more convenient dosing schedules, cell-stimulating factor
that has changed the dosing regimen for chemotherapy.
The approach to practice medicinal chemistry has developed from an empirical one
involving organic synthesis of novel compounds, largely based on a modification of functional
groups in the known structures possessing known activity.
Mastering and understanding such a breadth of the subject is not a simple task, but by the
same token, there is ample intellectual stimulation in understanding to fight against the disease at
the molecular level and in designing molecule ‘soldiers’ to win the battle.
General Information
3
Chapter
General
Information
This chapter includes some basic information the pharmacist should know about.
1.1 ERRORS
Error is defined as the difference between the measured value and actual value.
Types of errors (Classification of Errors)
Errors can be classified into the following categories:
1. Personal error,
2. Systematic error, and
3. Random error
1.1.1 Personal Error
An error which occur due to a faulty procedure adopted by the person; E.g., loss of
precipitate during filtration, etc.
1.1.2 Systematic Error (Determinate Error)
The given error arises due to the defect in measurement. It is also called zero error. It may
be positive or negative in nature; E.g., instrumental error.
1.1.3 Random Error (Non-systematic/Indeterminate Error)
The given error occurs due to the sudden change in experimental conditions. It is also called
an accidental error; E.g., changes in temperature, humidity, etc.
1.2 ACCURACY
Accuracy is the measure of the deviation of the measured value and true value or the
closeness of a measurement to its true value.
1
4
A Textbook of Pharmaceutical
Chemistry
1.3 PRECISION
Precision is the measure of agreement of experimental measurements with each other or the
agreement between two or more measurements that have been made in the same way.
1.4 SIGNIFICANT FIGURES (SIGNIFICANT DIGITS)
Significant figures are the digits expressing results of a calculation involving measurements
such that only the last digit is uncertain.
Rules followed in deciding significant digits are given below:
1. All nonzero digits are significant. (2.4567)
2. Leading zero (left-sided) i.e., zero before nonzero digit is not significant. (0.0021)
3. All zeros to the right of the decimal are significant. (2.6000)
4. All zeros in between nonzero digits are significant. (4.0025)
5. Zeros only to show the position of decimal points is not significant.
1.4.1 Rounding of Figures
1. If the given digit to be discarded is 4 or less, the value of the last digit is not changed.
(2.4367 is rounded to two digits is 2.4)
2. If the given digit to discarded is 5 or greater than 5, the value of the last digit is increased
by 1. (1.7456 is rounded to be 1.75)
1.5 IMPURITIES
Any compound is said to be impure if it is having foreign matter. The presence of an
impurity in any pharmaceutical product leads to a decrease in quality, potency, purity, and shelf
period.
1.5.1 Sources of Impurities
(i) Raw materials
(ii) Method of manufacture
(iii) Product instability (chemical, physical)
(iv) Contamination
(v) Cross-contamination
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