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Course Code: PHT1409
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Course Title: Pharmaceutical and Medicinal Chemistry –III
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Credits = 3
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L
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T
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P
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Semester: VI
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Total contact hours: 45
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2
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1
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0
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List of Prerequisite Courses
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Pharmaceutical and Medicinal Chemistry –II
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List of Courses where this course will be prerequisite
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Pharmaceutical and Medicinal Chemistry –IV, Pharmaceutical and Medicinal Chemistry –V
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Description of relevance of this course in the B. Pharm. Program
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To train the students with respect to basics of Central Nervous System drugs, Cholinergic and Adrenergic drugs, Analgesics, Non-Steroidal Anti-inflammatory Drugs
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Sr. No.
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Course Contents (Topics and subtopics)
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Reqd. hours
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Studyofthefollowingclassesofdrugs withrespecttotheirclassification,chemical nomenclature, structure including stereochemistry, generic names, chemistry, physicochemical properties,SAR,metabolism,molecularmechanism ofactionandsynthesisandintroductionto rational development, if any.
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1
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Drugs Affecting the Central Nervous System
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General introduction to biogenic amines and other biomolecules involved in neurotransmission
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2
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General anaesthetics: Inhaled general anesthetics and Intravenous general anesthetics.
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1
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Sedatives and hypnotics: Benzodiazepines, Non-benzodiazepine, Barbiturates, Misc.
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3
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Antiseizure drugs or anticonvulsant agents: Clinical drugs and newer agents
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2
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Antidepressants: Selective norepinephrine reuptake inhibitors (SNRIs),Selective 5-HT reuptake inhiitors (SSRIs), Nonselective reuptake inhibitors (NSRIs), Dopamine and norepinephrine reuptake inhibitors (DNRIs), Serotonin antagonist/reuptake inhibitors (SARIs), nonadrenergic specific serotonergic antidepressants (NaSSAs), monoamine oxidase inhibitors (MAOIs), Mood stabilizers.
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5
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Antipsychotics: phenothiazes, thioxanthines, benzamide, benzapines, benzisoxazole and benzisothiazoles, misc. agents.
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2
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Anxiolytics: Benzodiazapines, Misc agents.
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1
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Hallucinogens, Stimulants and related drugs of abuse or analeptics, xanthines, psychedelics: Non classical Hallucinogens- cannabinoids, classical hallucinogens- Indolealkylamines, phenylalkylamines, Central stimulants-amphetamine related agents, cocaine related agents.
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2
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Drugs used to treat neuromuscular disorder: Antiparkinsonian and spasmolytic agents.
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1
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Drugs affecting serotonergic neurotransmission- drugs for migrane, Irritable Bowel Syndrome, Anitemetic agents.
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2
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2
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Cholinergic Drugs or Drugs affecting cholinergic neurotransmission:
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General aspects of cholinergic receptor and acetylcholine, Acetyl choline mimetics- muscarainic agonist or cholinergic agonists, Anticholine esterases, Acetylcholine antagonists, muscrinic antagonists, Neuromuscular blocking agents.
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5
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Drugs for the treatment of Alzheimer’s disease
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1
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3
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Adrenergic Drugs or drugs affecting adrenergic neurotransmission:
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General aspects of adrenergic receptors and Non-selective adrenergic agonists- nor- epinephrine and epinephrine.
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2
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Selective α1-adrenergic agonists and α2-adrenergic agonists, β1 and β2- adrenergic agonists, Mixed-acting sympathomimetics
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3
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Non-selective and Selective α-adrenergic antagonists, β-adrenergic antagonists, Mixed α/β-adrenergic antagonists: Ergot alkaloids
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4
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4
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Drug Receptor Interactions Introduction:
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Understand concept of Drug - Receptor interactions; Affinity of drug for receptor- role of chemical bonding and conformation
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1
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Understand concept of Stereochemistry and Bioisosterism in Drug-Receptor interactions
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1
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Classification of different families of receptors and enzymes
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2
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5
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Analgesics: Opoid or narcotic analgesics: µ-agonists, other analgesics, mixed agonist/antagonist analgesics, µ-antagonists, Antidiarrheal agents, Cough suppressants, anti-tussives narcotic and others.
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5
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List of Text Books/ Reference Books
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1
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Foye, William O. Foye's principles of medicinal chemistry. Edited by Thomas L. Lemke, and David A. Williams, 6th edition, Lippincott Williams & Wilkins, 2008.
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2
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Wilson, Charles Owens, and Ole Gisvold, Textbook Of Medicinal And Pharmaceutical Chemistry, 11th edition, Lippincott Williams & Wilkins, Philadelphia, 2004
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3
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Donald J. Abraham, David P. Rotella, Burger's Medicinal Chemistry, Drug Discovery and Development, 7th Edition, 8 Volume Set, John Wiley & Sons-New Jersey,2010
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4
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Remington, Joseph Price. Remington: The science and practice of pharmacy. Edited by David B. Troy, and Paul Beringer. Vol. 1. Lippincott Williams & Wilkins, 2006.
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5
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Iyer R. P, Degani M. S., Synthesis Of Drugs: A Synthon Approach, 2nd edition, Vol-1, Sevak Publications Pvt. Ltd., 2008
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6
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Axel Kleemann and Jürgen Engel, Pharmaceutical Substances: Synthesis, Patents, Applications (N-Z) Kleemann 4th edition, Thieme, 2011
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7
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Lednicer, Daniel. The organic chemistry of drug synthesis. Vol. 7. John Wiley & Sons, 2007.
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8
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R. B. Silverman & Holladay, The Organic Chemistry of Drug Design And Drug Action. 3rd edition, Elsevier Publication, 2014
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Course Outcomes (students will be able to…..)
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1
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Draw and understand structures and write IUPAC names of structures (includes 3D structures) and classify drugs
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2
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Explain mechanism of action of drugs at molecular level & understand and apply the concepts of SAR.
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3
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Comprehend drug-receptor interactions
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4
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Predict the synthetic routes for simple drugs
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Note: The above course outcomes are related to Central Nervous System drugs, Cholinergic drugs, Adrenergic drugs and Analgesics
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