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- •Preface
- •Contents
- •1.1 Introduction
- •1.3 Drug Discovery: A Historical Perspective
- •1.4 Drug Discovery and Development Processes
- •1.5 Modern Approach of Research and Development Strategies
- •Questions
- •2.1 Introduction
- •2.2 Retrosynthetic Analysis: The Concepts
- •1.6 Role of Natural Products in Target Identification
- •1.7 Bioisosterism
- •1.8 Role of Stereochemistry in Drug Discovery
- •2.3 Basic Synthetic Strategies: General Approaches Used for Synthesis Problems
- •2.4 Retrosynthetic Analysis: Other Simplification Rules
- •2.5 Retrosynthetic Analysis: Synthetic Impropriety to Avoid
- •Questions
- •3.1 Introduction
- •3.2 Classification
- •3.3 Mechanism of Action
- •3.4 Analgesic Agents
- •3.5 Anti-Inflammatory Drugs
- •3.6 Opioid Receptor Discovery
- •3.7 Aspirin
- •3.8 Ibuprofen
- •3.9 Paracetamol
- •3.10 Diclofenac
- •Questions
- •4.1 Introduction
- •4.2 Antibacterial Agents
- •4.3 Antifungal Agents
- •4.4 Chloramphenicol
- •4.5 Sulfonamides
- •4.6 Sulfamethoxazole
- •4.7 Sulfacetamide
- •4.8 Trimethoprim
- •Questions
- •5.1 Introduction
- •5.2 Drugs Acting on CNS and Peripheral Nervous System (PNS)
- •5.3 Barbiturates
- •Questions
- •6.1 Introduction
- •6.2 Cardiovascular Drugs
- •6.3 Organic Nitrates
- •Questions
- •7.1 Introduction
- •7.2 The Organism
- •7.3 Drug Testing Systems
- •7.4 Chemotherapy
- •7.5 Classification of Leprosy and the Clinical Symptoms
- •7.6 Leprosy Co-existing Factors
- •7.7 Dapsone
- •7.8 Clofazimine (Lamprene)
- •7.9 Solapsone (Sulphetrone)
- •7.10 Ethionamide (Ethionamidum)
- •7.11 Rifampicin (Rifampin)
- •7.12 Clarithromycin
- •7.13 Minocycline
- •7.14 Other Sulfone Derivatives Active Against Leprosy
- •7.15 Treatment of Leprosy Using Chaulmoogra Oil
- •7.16 WHO Recommended Chemotherapeutic Regimens
- •Questions
- •8.1 Introduction
- •8.2 Structure of Viruses
- •8.3 Life Cycle of Viruses
- •8.4 Antiviral Drug Targets
- •8.5 Antiviral Drugs Acting Against RNA Viruses: HIV
- •8.6 Acquired Immune Deficiency Syndrome (AIDS)
- •Questions
- •9.1 Introduction
- •9.2 Life Cycle of the Malaria Parasite
- •9.3 Antimalarial Drugs
- •9.4 National Drug Policy on Malaria
- •9.5 WHO Guidelines for the Treatment of Malaria
- •Questions
- •10.1 Introduction
- •10.2 Production of Ethyl Alcohol and Citric Acid
- •10.3 Production of Antibiotics
- •10.4 Production of Lysine
- •10.5 Production of Glutamic Acid
- •10.6 Production of Vitamin B2 (Riboflavin)
- •10.7 Microbial Production of Vitamin B12
- •10.8 Production of Vitamin C (Ascorbic Acid)
- •Questions
- •11.1 Medicinal Importance of Haldi or Curcumin (Curcuma longa)
- •11.2 Medicinal Importance of Neem (Azadirachta indica)
- •11.3 Medicinal Value of Vitamin C (Ascorbic acid)
- •11.4 Medicinal Importance of Ranitidine
- •11.5 Medicinal Importance of Ginger (Zingiber officinale)
- •11.6 Medicinal Importance of Tulsi (Ocimum tenuiflorum)
- •11.7 Medicinal Importance of Garlic (Allium sativum)
- •11.8 Medicinal Importance of Ajwain (Trachyspermum ammi)
- •Questions
- •Abbreviations
- •Bibliography
- •Index

382 Pharmaceutical Chemistry
673. Skin pigmentation is a feature of all, except:
(a) Nelson syndrome (b) Hemochromatosis
(c) Cushing’s syndrome (d) Melphalan therapy
674. The incubation period of chicken pox is:
(a) 2 weeks (b) 1 week
(c) 3 days (d) 2–3 weeks
675. Who is known as the father of medicine?
(a) Aristotle (b) Dioscorides
(c) Hippocrates (d) Galen
676. Which of the following statements best describes retrosynthesis?
(a) The design of reaction conditions such that an equilibrium reaction is pushed
towards the products rather than the starting materials.
(b) A strategy used to design a synthesis of a target molecule by working back
from the target to simple starting materials.
(c) The design of a synthetic scheme using cheap, traditional reagents, rather than
expensive modern reagents.
(d) The reaction conditions required to convert the product of a reaction back to the
original starting materials.
677. Which of the following statements best describes a synthon?
(a) A hypothetical structure that would result in a given reaction if it existed.
(b) A key intermediate in a reaction sequence.
(c) A synthetic reagent used in a reaction.
(d) A transition state involved in a reaction mechanism.
678. Which of the following statements best describes a disconnection in retrosynthesis?
(a) A disconnection describes the reaction conditions required to split a target
structure into simpler molecules.
(b) A disconnection identifies retrosynthetic stages which would not be feasible in
the corresponding synthesis.
(c) A disconnection involves identifying stages where a bond is split in the
corresponding synthesis.
(d) A disconnection involves a theoretical disconnection of a bond in a target
structure in order to identify simpler structures that could be linked through
the formation of that bond.

Abbreviations
AcOH : Acetic acid
AIDS : Aquired immune deficiency syndrome
HIV : Human immunodeficiency virus
ACE : Angiotensin-converting-enzyme
ASC : p-Acetamidobenzene sulfonyl chloride
ATP : Adinosine triphosphate
ADME : Absorption-distribution-metabolism-excretion
AIDS : Acquired immunodeficiency syndrome
AMI : Acute myocardial infarction
AZT : Zidovudine
BBB : Blood brain barrier
BI : Bacteriological index
BzCl : Benzoyl chloride
cGMP : Cyclic guanosine monophosphate
dGTP : Deoxyguanosine triphosphate
CHF : Congestive heart failure
CMI : Cell mediated immune
CNS : Central nervous system
COX : Cyclooxygenases
CQ : Chloroquin
CYP : Cytochrome P450
CYS : Cystein
DHF : Dihydrofolic acid
DHFR : Dihydrofolate reductase
DNA : Deoxyribonucleic acid
DOPA : Dihydroxyphenylalanine
Et : Ethyl

384 Pharmaceutical Chemistry
FAAH : Fatty acid amide hydrolase
FDA : Food and Drug Administration
GABA : J-Aminobutyric acid
GIT or GI : Gastrointestinal tract
GTP : Guanosine 5’-triphosphate
HBA : H-Bond acceptor
HBD : H-Bond donor
HIV : Human Immunodeficiency virus
HSV : Herpes simplex virus
HTS : High throughput screening
IDDM : Insulin dependent diabetes mellitus
LTHC : Lipophilic tetrahydrocannabinol
Me : Methyl
MeI : Methyl iodide
MADDS : Mono-acetylated metabolite
MAO : Monoamine oxidase
nAChRs : Nicotine acetylcholine receptors
NADPH : Nicotinamide adenine dinucleotide phosphate
NSAIDs : Non-steroidal anti-inflammatory drugs
NE : Norepinephrine
NO : Nitric oxide
PABA : p-Amino benzoic acid
PG : Prostaglandin
PK : Pharmacokinetics
Ph : Phenyl
PSA : Polar surface area
Pi : Partition coefficient
PTGS : Prostaglandin
QSAR : Quantitative structure activity relationships
RA : Retrosynthetic analysis
RC : Respiratory centre
RDT : Rapid diagnostic test
RNA : Ribonucleic acid
RT : Room temperature
SAR : Structure activity relationships
SMZ or SMX : Sulfamethoxazole

SPR : Structure property relationship
SSRI : Selective serotonin reuptake inhibitor
TCA : Tricyclic antidepressant
THF : Tetrahydrofolic acid
TMP : Trimethoprim
TL : Tuberculoid leprosy
UDP : Uridine diphosphate
VMC : Vasomotor centre
WHO : World Health Organization
Abbreviations 385


Bibliography
1. Aggarwal, B.B., Bhatt, I.D., Ichikawa, H., Ahn, K.S., Sethi, G., Sandur, S.K.,
Sundaram, C., Seeram, N. and Shishodia, S. (2006). Curcumin - Biological and
Medicinal Properties. 7034_book.fm (Page 297).
2. Ahmed, B. (2007). Medicinal Chemistry: Cardiovascular Drugs. Dept. of
Pharmaceutical Chemistry. Jamia Hamdard, New Delhi.
3. AIDS Info. (2009, July). Approved medications to treat HIV infection. Accessed
May, 2011. The National Institutes of Health. http://aidsinfo.nih.gov/contentfiles/
ApprovedMedstoTreatHIV_FS_en.pdf.
4. AIDS Info. (2008, December). HIV and its treatment: What you should know.
Accessed May, 2011. The National Institutes of Health. http://aidsinfo.nih.gov/
contentfiles/HIVand ItsTreatment_cbrochure_en.pdf.
5. Antileprosy Drugs. (1971). British Med. J. pp. 174-176.
6. Beale, J.M. and Block, J.H. (2011). Textbook of Organic Medicinal and Pharmaceutical
Chemistry. Baltimore, MD: Lippincott Williams and Wilkins: A Wolters Kluwer
Company.
7. Bhanja, C., Chakroborty, S. and Jena, S. (2014). Synthesis planning of potent
antimigraine drug Sumatriptan using retrosynthetic analysis. Asian Journal of
Pharmaceutical Analysis and Medicinal Chemistry. 2(3): 168-175.
8. Chauhan, B., Kumar, G. and Ali, M. (2012). A Review on Phytochemical Constituents
and Activities of Trachyspermum Ammi(l.) Sprague fruits. Am. J. Pharm. Tech. Res.
2(4): 329-340.
9. Chhibber, S. and Sharma, N. (2014). Medicinal and therapeutical potential of neem
(Azadirachta indica). Inter. J. Sci. Res. 4(5): 1-5.
10. Collins, S., Clayden, P., Konov, S.K. et al. (2007). Treatment training for advocates,
Vitology, HIV, and viral load (Chap. 2). Accessed May, 2011. http://www.i-base.
info/manual/en/2-14.html.
11. Czapinski, P., Blaszczyk, B. and Czuczwar, S.J. (2005). Mechanisms of action of
antiepileptic drugs. Cur. Topics in Med. Chem. 5: 3-14.

388 Pharmaceutical Chemistry
12. Delgado, I.N. and Remers, W.A. (1998). Wilson & Gisvold’s: Textbook of Organic
Medicinal and Pharmaceutical Chemistry. (10th ed.). New York: Lippincott Raven
Publishers.
13. Doelle, H.W., Rokem, S. and Berovic, M. (Eds.). (2009). Biotechnology: Encyclopaedia
of Life Support Systems. Sanchez-Riera, F. Production of Organic Acids. Vol. V: 100.
14. Doelle, H.W., Rokem, S. and Berovic, M. (Eds) (2009). Biotechnology: Encyclopaedia
of Life Support Systems. Gutierrez, S., Casqueiro, J. and Martin, J.F. Production of
Antibiotics. Area of Microbiology, University of Leon, Spain. Vol. V : 126.
15. Edward, G. (2001). Antimalarial chemotherapy: Mechanisms of action, resistance
and new directions in drug discovery. Br. J. Clin. Pharmacol. 52(4): 464.
16. Engelman, A. and Cherepanov, P. (2012). The structural biology of HIV-1:
Mechanistic and therapeutic insights. Nat. Rev. Microbiol. 10: 279-290.
17. Fasinu, P.S., Tekwani, B.L., Nanayakkara, N.P.D, Avula, B. et al. (2014).
Enantioselective metabolism of primaquine by human CYP2D6. Malaria Journal. 13:
507.
18. Feng, P.C.C., Fenselau, C.C. and Jacobson, R.R. (1981). Metabolism of clofazimine
in leprosy patients. Drug Metabolism and Disposition. 9: 521-524.
19. Feng, P.C.C., Fenselau, C.C. and Jacobson, R.R. (1982). A new urinary metabolite of
clofazimine in leprosy patients. Drug Metabolism and Disposition. 10: 286-288.
20. Geyer, M. (2001). Antimalarial drug combination therapy report of a WHO technical
consultation. WHO, Geneva, Switzerland.
21. Ghosh, A.K. (2011). Zingiber officinale: A natural gold. Int. J. Pharma & Bio Sci. 2(1):
283-294.
22. Glossary of terms used in Medicinal chemistry. http://www.chem.qmul.ac.uk/
iupac/medchem/ix.html#s5.
23. Guidelines for the treatment of Malaria (3rd ed.). WHO (2015).
24. Hooper, M. (1987). The medicinal chemistry of anti-leprosy drugs. Chem. Soc. Rev.
16: 437–465.
25. Hughes, J.P., Rees, S., Kalindjian, S.B. and Philpott, K.L. (2011). Principles of early
drug discovery. British J. Pharmacology. 162: 1239–1249.
26. Hughes, W.T. (1998). Use of Dapsone in the prevention and treatment of Pneumocystis
carinii Pneumonia: A Review. Clinical Infectious Diseases. 27: 191–204.
27. Hulzebos, E.M., Janssen, P.A.H., Maslankiewicz, L., Meijerink, M.C.M., Muller,
J.J.A., Pelgrom, S.M.G., Verdam, L. and Vermeire, T.G. (2001). The application of
structure activity relationships in human hazard assessment: A first approach.
RIVM Report No. 601516008.
28. Insel, P.A. (1990). Analgesic-antipyretics and anti-inflammatory agents: Drugs
employed in the treatment of rheumatoid arthritis and gout. In A.G. Gilman, T.
Rall, and A. Nies.

Bibliography 389
29. Izawa, K. and Shiragami, H. (1998). Practical syntheses of antiviral nucleosides.
Pure & Appl. Chem. 70(2): 313-318.
30. Kalapathy, U., Proctor, A. and Shultz, J. (2000). A simple method for production of
pure silica from rice hull ash. Biores. Technol. 73(3): 257-262.
31. Kamath, S.R. and Proctor, A. (1998). Silica gel from rice husk ash: Preparation and
characterization. Cereal Chem. 75: 484-487.
32. Kar, A. (2005). Medicinal Chemistry (3rd
ed.). New Delhi: Wiley Eastern Ltd.
33. Kaur, K., Jain, M., Kaur, T. and Jain, R. (2009). Antimalarials from nature. Bioorg.
Med. Chem. 17(9): 3229-3256.
th
34. Katzung, B.G. (2004). Basic and Clinical Pharmacology (9
ed.). McGraw-Hill.
35. Kerns, E. H. and Di, L. (2008). Drug-like Properties: Concepts, Structure Design and
Methods–from ADME to Toxicity Optimization. USA: Elsevier Inc.
36. Kloner, R.A. (2009). A salute to our founding Editor-in-Chief, Bramah N. Singh
(MD, Dphil, DSc, FRCP), J. Cardiov. Pharmacol. Therapeutics. 14(3): 154-156.
37. Kubinyi, H. (2002). Chemical similarity and biological activities. J. Braz. Chem. Soc.
13(6): 717-726.
38. Lakshmi, P.V. and Mangala, D.S. (2011). Fermentative production of L-Glutamic
acid. Inter. J. Advan. Biotechnol. Res. 2(3): 376-381.
/HYLQ -, DQG /DXIHU 6 $QWLLQÁDPPDWRU\ GUXJ GLVFRYHU\ RSC Drug
Discovery Series, No. 26.
40. Loscher, W. and Rogawski, M.A. (2012). How theories evolved concerning the
mechanism of action of barbiturates. Epilepsia. 53(8): 12–25.
41. Majewski, H. (Ed.). Pharmacology–Encyclopaedia of Life Support Systems. Ruffolo,
R.R., Walsh, F.S. Jr. and Feuerstein, G.Z. Drug Discovery. pp. 311.
42. Mane, P.B., Antre, R.V. and Oswal, R.J. (2012). Antileprotic Drugs: An Overview.
Int. J. Pharm. Chem. Sci. 1(2): 738-746.
43. Mayer, D., Fabiano-Tixier, A-S., Petitcolas, E., Hamieh, T., Nehme, N., Ferrant, C.,
Fernandez, X. and Chemat, F. (2014). Chemical composition, antibacterial and
antioxidant activities of six essential oils from the Alliaceae family. Molecules. 19:
20034-20053.
44. McKinney, J.D., Richard, A., Waller, C., Newman, M.C. and Gerberick, F. (2000).
The practice of structure activity relationships (SAR) in toxicology. Toxicol. Sci. 56:
8-17.
45. Muniz, C.C., Zelaya, T.E.C., Esquivel, G.R. and Fernandez, F.J. (2007). Penicillin
and Cephalosporin production: A historical perspective. Rev. Latinoam. Microbiol.
49(3-4): 88-98.
46. Myers, R.S. (2006). Immunizing and Antimicrobial Agents. Chapter VI: Antifungal
Agents. University of Washington. (MEDCH-401).

390 Pharmaceutical Chemistry
47. “National drug policy on Malaria 2013” by Directorate of National Vector Borne
Disease Control Programme, Directorate General of Health Services, Ministry of
Health and Family Welfare, Delhi, India.
48. Nikolova, N. and Jaworska, J. (2003). Approaches to Measure Chemical Similarity–A
Review. QSAR Comb. Sci. 22: 1006-1026.
2]JXO<FHO 6 7ROD\ 0 (UGDş 6 DQG 7XUND\ 6 0DJQHVLXP VLOLFDWH
synthesis from rice husk ash. J. Am. Oil Chem. Soc. 81: 619-620.
50. O’Neill, P.M., Barton, V.E., Ward, S.A. and Chadwick, J. (2012). 4-Aminoquinolines:
Chloroquine, Amodiaquine and next-generation analogues. In: Treatment and
Prevention of Malaria, H. M. Staines & S. Krishna (Eds.). DOI 10.1007/978-3-03460480- 2_2, # Springer Basel AG.
51. Pattanayak, P., Behera, P., Das, D. and Pand, S.K. (2010). Ocimum sanctum Linn. A
reservoir plant for therapeutic applications: An overview. Pharmacogn Rev. 4(7):
95-105.
52. Pharmacopoeia of India (2011). Govt. of India. Ministry of Health, Delhi.
53. Premkumar, R. (2010). The history of a leprosy sanatorium in India. A literature
review. Lepr. Rev. 81: 150–159.
54. Qin, F. and Xu, H. (2008). Active compounds in gingers and their therapeutic use in
complimentary medication. Med. Arom. Plant Sci. Biotech. 2(2): 72-78.
55. Rainsford, K.D. (2009). Ibuprofen: Pharmacology, efficacy and safety.
Inflammopharmacol. 17: 275–342.
56. Rainsford, K.D. (2007). Anti-inflammatory drugs in the 21st century. R.E. Harris
(Ed.). Inflammation in the Pathogenesis of Chronic Diseases. Springer. pp. 3-27.
57. Saifi, M.A., Beg, T., Harrath, A.H., Altayalan, F.S.H. and Quraishy, S.A. (2013).
Antimalarial drugs: Mode of action and status of resistance. Afr. J. Pharmacy &
Pharmacol. 7(5): 148-156.
58. Schlitzer, M. (2008). Antimalarial drugs–What is in use and what is in the pipeline.
Arch. Pharm. Chem. Life Sci. 341: 149–163.
59. Seiter, J., Fass, M., Stanley, E. and Waterman, M. (2009). HIV/AIDS: Biology and
treatment. Biol. Intern. 49: 86-95.
60. Sharma, P., Tomar, L., Bachwani, M. and Bansal, V. (2011). Review on Neem
(Azadirachta indica): Thousand problems one solution. Intern. Res. J. Pharma. 2(12):
97-102.
61. Soccol, C.R., Vandenberghe, L.P.S., Rodrigues, C. and Pandey, A. (2006). New
perspectives for citric acid production and application. Food Technol. Biotechnol.
44(2): 141–149.
62. Survase, S.A., Bajaj, I.B. and Singhal, R.S. (2006). Biotechnological Production of
Vitamins. Food Technol. Biotechnol. 44(3): 381–396.
63. Taylor, P. (Ed.). Goodman and Gilman’s The Pharmacological Basis of Therapeutics.
New York: Pergamon. pp. 638-681.

Bibliography 391
64. Thomas, G. (2003). Fundamentals of Medicinal Chemistry. England: John Wiley &
Sons Ltd.
65. Tian, W., Shen, J., Zhou, M., Yan, L. and Zhang, G. (2012). Dapsone hypersensitivity
syndrome among leprosy patients in China. Lepr. Rev. 83: 370–377.
66. Watson, D.G. (2011). Pharmaceutical Chemistry. Elsevier Ltd.
67. WHO study groups on “Chemotherapy of leprosy”. (1994). WHO Technical Report
Series 847, Geneva.
68. Williams, D.A. and Lemke, T.L. (2002). Foye’s Principles of Medicinal Chemistry.
(5th ed.). Philadelphia: Lippincott Williams & Wilkins.
69. Vaughan Williams, E.A. (1970). Classification of antiarrhythmic drugs. In:
Symposium on Cardiac Arrhythmias (Eds. Sandoe, E., Flensted-Jensen, E. and
Olsen, K.H.). Denmark: Astra, Elsinore.
70. Venkatesan, K. (1989). Clinical pharmacokinetic considerations in the treatment of
patients with leprosy. Clinical Pharmacokinetics. 16: 365-386.
71. Viggosson, A.B. (2011). A review of the first specific anti-viral agent: Acyclovir.
Uppsala University, Sweden.
72. Xu, H. and Agrafiotis, D.K. (2002). Retrospect and prospect of virtual screening in
drug lead discovery. Curr. Topics Med. Chem. 2: 1305-1320.
Websites:
https://www.wavefun.com/products/books/Chapter1.pdf.
http://www2.chemistry.msu.edu/courses/cem850/F12_WULFF/SM-28.pdf.
http://ramsey1.chem.uic.edu/chem232/page7/files/Chem%20232%20
Synthesis%201.pdf.
http://watcut.uwaterloo.ca/webnotes/Pharmacology/rnaRibosomalAntibiotics.
html.
http://www.h1n1.ro/Sulfonamide.html.
http://www.hampsteadscience.ac.uk/TheMedicinalChemistryofAntibiotics.pdf.
http://www.hull.ac.uk/php/chsanb/BactWeb/Antiinfectives.pdf.
http://www.inchem.org/documents/pims/pharm/pim181.htm.
https://www.erowid.org/archive/rhodium/chemistry/diazepam.html.
http://watcut.uwaterloo.ca/webnotes/Pharmacology/metabolismOverview.html.
http://www.pdr.net/full-prescribing-information/dapsone?druglabelid=261.
http://faculty.swosu.edu/scott.long/phcl/antivirl.htm.
www.mmv.org.
http://watcut.uwaterloo.ca/webnotes/Pharmacology/microbesAntivirals.html.
http://www.malariasite.com/malariadrugs.
http://www.genomicglossaries.com/content/drug_discovery_gloss.asp.
www.pdb.org and info@rcsb.org.
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