LESSON PLAN KLESCOPH DR.V.S.MADDI/SHRI.S.N.

MAMLEDESAI SUBJECT: MEDICINAL CHEMISTRY-I DEPARTMENT: PHARMACEUTICAL CHEMISTRY

CHAPTER: INTRODUCTION Number of hours required as per RGHUS syllabus: 2 Number of hours required as per lesson plan : 2 Prerequisite: Student needs to have fundamentals of Organic Chemistry, synthetic manipulative skills Objective: a. To teach development of medicinal chemistry b. To teach fundamental principles of drug therapy Resources: a. Black board and chalk pieces b. OHP References: 1.Wilson and Giswolds textbook of organic and medicinal chemistry 2.William O Foye, Principles of medicinal chemistry 3. Burgers medicinal chemistry vol 1,2,3,4&5 4. Kadam,Textbook of medicinal chemistry vol I&II

Model questions: 5 marks type 1. 2. Give a brief account of development of medicinal chemistry. Enumerate fundamental principles of drug therapy with examples.

CHAPTER: PHYSICOCHEMICAL PROPERTIES AND PRINCIPLES OF DRUG DESIGN Number of hours required as per RGHUS syllabus :8 Number of hours required as per lesson plan :8 Pre requisite: Student needs to possess basic idea about various physical and chemical parameters like solubility, ionization, pH, redoxpotential, hydrogen bonding ,isomerism etc Student should know the origin and strengths of various electrostatic forces Objectives: To make student understand a. how these physicochemical parameters influence the course of drug action viz absorption,distribution and excretion b. the concept of isosterism and its role in drug design c. the effect of optical and geometrical isomers on pharmacodynamics of drugs d. the general principles of drug action and the forces involved in drug receptor interaction

Resources: a. black board and chalk pieces b. OHP References: 1.Wilson and Giswolds textbook of organic and medicinal chemistry 2.William O Foye, Principles of medicinal chemistry 3. Burgers medicinal chemistry vol 1,2,3,4&5 4. Kadam,Textbook of medicinal chemistry vol I&II Model questions: 2 marks type 1. 2. Give a note on isosterism and biological activity (2M) Write briefly on redox potential (2M)

5 marks type: 3. chelation. 4. molecules. 5. 6. with 7. 8. 9. receptor 10. Describe how solubility ,partition coefficient and hydrogen bonding influence drug action giving one example in each case. Discuss drug receptor interaction and the role of binding forces suitable examples for the importance of stereochemistry. Discuss how ionization influences biological activity. Explain the importance of isosterism in biological activity of drugs. Explain the theretical aspects of drug design with reference to drug interaction. Give the structures of drugs that exhibit a. Geometrical isomerism Explain the Ferguson theory on physical properties of drug Describe how drug action is influencedby protein binding and

b. optical isomerism. 10 marks type: 11. examples 12. biological Explain how the following properties of drug molecules affect their biological activity; substantiate your answer with suitable a.Protein binding b.Isomerism c.complexation Discuss the various physicochemical properties affecting the activity of drugs

CHAPTER: DRUG METABOLISM Number of hours required as per RGHUS syllabus :4 Number of hours required as per lesson plan : 4 Pre requisite: Student must have the knowledge of various biochemical processes taking place in the body with the help of enzymes Basics of functional group transformation in Org. Chem. Objective: To teach the student a. 1.Drug biotransformation and sites of it b. 2.factors affecting drug metabolism c. 3.routes of biotransformation and its consequences d. 4.toxicities exhibited by drug metabolites e. 5.Textbook of pharmacology- tripathi Resources: a. a.black board and chalk pieces b. b.OHP

References: 1. 2. 3. 4. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II

Model questions: 2 marks type 1. 2. 3. Write briefly on sites of biotransformation. Write a note on Glutathione conjugation. Discuss the biotransformation of paracetamol.

5 marks type 4. Write briefly on the general pathways of drug metabolism. 5. Describe the role of cytochrome P-450 monooxygenase in oxidative biotransformation. 6. Describe the factors that affect drug metabolism. 7. Explain first pass metabolism of drugs with suitable examples 8. Discuss the importance of conjugation reaction in drug metabolism giving specific examples. 10 marks type 9. Describe in detail the drug metabolism giving emphasis on various pathways

CHAPTER: GENERAL ANAESTHETICS Number of hours required as per RGHUS syllabus :4 Number of hours required as per lesson plan : 4 Pre requisite: The student should have basic idea of The physiology of CNS The physiology of nerve transmission Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions 2 marks type 1. 2. Note on dissociative anaesthetics Write a note on general anaesthetics

5 marks type 3. 4. Write briefly on inhalation anaesthetics Write the structures and uses of ultra short acting barbiturates

CHAPTER: ANXIOLYTICS,SEDATIVES AND HYPNOTICS Number of hours required as per RGHUS syllabus :6 Number of hours required as per lesson plan : 6 Pre requisite: Student should have idea of working of brain Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs e. classification Resources:

a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- Tripathi

Model Questions 2 marks type 1. 2. 3. Discuss Amides and imides as sedatives and hypnotics. How do you distinguish sedatives from anxiolytics? Explain with suitable examples. Outline the synthesis of methohexital sodium.

5 marks type: 4. 5. 6. 7. 8. 9. Give a list of anxiolytic agents along with their structures. Discuss briefly about anxiolytic agents. Explain the mechanism of action of benzodiazepines as minor tranquillisers. Describe the synthesis and uses of diazepam and chlordiazepoxide. Aldehydes and their derivatives with sedative and hypnotic activity. Describe how structural changes influence duraration of action in malonylureas. 10 marks type

10.

Classify barbiturates with examples. Discuss their SAR. write the synthesis of Phenobarbital (10M)

CHAPTER: SKELETAL MUSCLE RELAXANTS AND DRUGS USED IN SPASTICITY Number of hours required as per RGHUS syllabus :2 Number of hours required as per lesson plan : 2 Pre requisite: The student should have the knowledge of physiology of skeletal muscle contraction and relaxation Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions 2 marks type 1. 2. 3. Outline the synthesis of meprobamate. Write a note on agents used in spasticity. Write the structure and uses of tybamate and mephensin.

5 marks type 4. Discuss about skeletal muscle relaxants.

CHAPTER: ANTICONVULSANTS

Number of hours required as per RGHUS syllabus :5 Number of hours required as per lesson plan : 5 Pre requisite: Student needs to know the anatomy and physiology of brain and impulse conduction through nerves Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs

e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions: 2 marks type 1. 2. Outline the synthesis of phenytoin. Give the structure and uses of any nonbarbiturates used as anticonvulsants. 5 marks type 3. Classify anticonvulsants. What structure is common to all of them? OR Write the chemical classification of drugs employed in the management of convulsive disorders. 4. 5. Write the name, structure and clinical uses of any five drugs used as anticonvulsants. Write two structures of five membered and six membered cyclic ureides with their applications.

6. Bring out the similarities in structure of various categories of anticonvulsants. Explain how bioisosterism is used in designing such drugs. CHAPTER: ADRENERGIC AND ADRENOLYTIC AGENTS Number of hours required as per RGHUS syllabus :9 Number of hours required as per lesson plan : 9

Pre requisite: The student should know ANS in particular Sympathetic nervous system, the neurotransmitters involved in it Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5

4. 5. 6.

Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions: 5 marks type 1. 2. 3. 4. Discuss the structural features and stereochemistry of ephedrine OR structural elucidation of ephedrine. Discuss adrenergic antagonists with suitable examples. Outline the biosynthetic pathway for adrenergic neurotransmitters. Enumerate the structural features essential for directly acting sympathomimetic agents.

10 marks type 5. write the structures of 5 -blocking agents.whatare their therapeutic applications?write the synthesis and uses of propranalol. 6. Give a list of -adrenergic receptor agonists and write their structures. Write the synthesis of terbutaline. 7. Explain the mechanism of action of adrenergic agents giving examples. Show the principal routes through which they are metabolized. Outline the synthesis of any one adrenergic agonist.

CHAPTER : CHOLINERGIC AND CHOLINERGIC BLOCKING AGENTS Number of hours required as per RGHUS syllabus :14 Number of hours required as per lesson plan : 9

Pre requisite : The student should know ANS in particular Parasympathetic nervous system, the neurotransmitters involved in it Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model questions: 2 marks type 1. 2. 3. Discuss the structures related to atropine. To what class malathion belongs?. Give the structure and uses of papaverine.

5 marks type

4. 5. 6.

What are cholinesterase inhibitors? How do they act? Give examples. Write a note on Ganglionic blocking agents. Give examples for curariform compounds. Add their uses.

10 marks type 7. 8. 9. Classify the agents acting on cholinergic nervous system giving structures to each class. Give the mechanism of action of parathion. Discuss the SAR of synthetic cholinergic blocking agents. Give the synthesis and uses of physostigmine. Discuss the structural elucidation of atropine.

CHAPTER: LOCAL ANAESTHETICS Number of hours required as per RGHUS syllabus :5 Number of hours required as per lesson plan : 5 Pre requisite: The student should know the physiology of impulse conduction through neurons Objective: a. To teach the student b. The concept c. development and SAR d. mechanism of action e. structure,nomenclature and syntheses of drugs f. classification Resources:

a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions 2 marks type 1. 2. Give any two structures of local anaesthetics. Explain the chemistry of cocaine.

5 marks type 3. Write the mechanism of action of local anaesthetics.

10 marks type 4. 5. Classify local anaesthetics giving two structures to each class. Give synthetic approaches for a.lidocaine b.benzocaine. Define local anaesthetics. give the SAR of aminobenzoicacid derivatives aslocal anaesthetics. CHAPTER: HISTAMINES AND ANTI HISTAMINIC AGENTS Number of hours required as per RGHUS syllabus :6

Number of hours required as per lesson plan : 6 Pre requisite: The student should know about storage secretion and actions of histamine Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions: 2 marks type 1. 2. Give the synthesis and uses of phniramine, Give the structure and uses of a.mecizine b.tripelenamine.

3.

write the therapeutic utility of antihistamines.

5 marks type 4. Write a note on H2 antagonists.

10 marks type 5. 6. Give the classification of antihistamines giving 2 structures to each class. Outline the synthetic route for a.diphenhydramine b.promethazine. Classify anti allergic drugs. Write the SAR of anti histamines.

CHAPTER: NARCOTIC ANALGESIC AGENTS Number of hours required as per RGHUS syllabus :5 Number of hours required as per lesson plan : 5 Pre requisite: The student needs to know the physiology of CNS Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs e. classification Resources: a. black board and chalk pieces b. OHP References:

1. 2. 3. 4. 5. 6.

Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions: 2 marks type 1. 2. What are antitussive agents? Give two structures. Give structures of two synthetic analgesic agents.

5 marks type 3. 4. Write a note on narcotic antagonists. Write the modification done by Small and Eddy on morphine.

10 marks type 5. Discuss briefly the chemical modifications made on morphine.

CHAPTER: ANTIINFLAMMATORY AGENTS Number of hours required as per RGHUS syllabus :4 Number of hours required as per lesson plan : 4 Pre requisite: The student needs to know the pathophysiology of inflammation and its mediators Objective: To teach the student a. The concept b. development and SAR c. mechanism of action

d. structure,nomenclature and syntheses of drugs e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions: 2 marks type 1. Write the structure and uses of Indomethacin and Ibuprofen.

5 marks type 2. 3. Give the synthesis for naproxen and phenylbutazone. Classify NSAIDS giving examples.

10 marks type 4. Give the detailed classification of anti-inflammatory agents giving examples to each class. Write their general mode of action.

CHAPTER: PROSTAGLANDINS AND OTHER EICOSANOIDS Number of hours required as per RGHUS syllabus :6 Number of hours required as per lesson plan : 6 Pre requisite : The student should know about biosynthesis of prostaglandins and other eicosanoids Objective: To teach the student a. The concept b. development and SAR c. mechanism of action d. structure,nomenclature and syntheses of drugs e. classification Resources: a. black board and chalk pieces b. OHP References: 1. 2. 3. 4. 5. 6. Wilson and Giswolds textbook of organic and medicinal chemistry William O Foye, Principles of medicinal chemistry Burgers medicinal chemistry vol 1,2,3,4&5 Kadam,Textbook of medicinal chemistry vol I&II Organic drug synthesis- Ledniser and Mitzsher vol 1&2 Textbook of pharmacology- tripathi

Model Questions: 1. 2. Give few examples of prostaglandins which have therapeutic significance. What are eicosanoids? Mention their significance.