COURSE SPECIFICATION - KKU · course specification male section medicinal chemistry 2 (pch 422) for...

Dept. of Pharmaceutical Chemistry, Medicinal Chemistry 2 (PCH 422)

KING KHALID UNIVERSITY

COLLEGE OF PHARMACY

DEPARTMENT OF PHARMACEUTICAL CHEMISTRY

COURSE SPECIFICATION

MALE SECTION

MEDICINAL CHEMISTRY 2 (PCH 422)

For

PHARMACEUTICAL SCIENCES / CLINICAL PHARMACY

BY

Dr. Kumar Venkatesan

Academic Session 1437-1438

1st Semester

(Semester No 371)

September 2016 - January 2017


COURSE SPECIFICATION

Course Title MEDICINAL CHEMISTRY 2

Course Code PCH 422

Credit Hours 3 (2 Theoretical hours +1 Practical hour)

Program(s) in which the course is

offered

BACHELOR OF PHARMACEUTICAL SCIENCES/ CLINICAL

PHARMACY, COLLEGE OF PHARMACY, KKU.

Name of faculty member responsible for

the course

Dr. Kumar Venkatesan Assistant Professor Department of Pharmaceutical chemistry College of Pharmacy-KKU, ABHA Phone Office: 0172417982 Email: [email protected] Mobile Ph.: 0505735246 Office:163/4/c

Lecture Timings Theory Day 1(Sunday): 02:00 – 2:50 PM Room No: C/5/40 Day 1(Sunday): 03:00 – 3:50 PM Room No: C/5/40 Section 96

Lecture Timings Practical Batch 1; Section 97; Day 4 (Wednesday)1 pm to 3 pm; Room Number - C\4\45 Batch 2; Section 98; Day 5 (Thursday)1 pm to 3 pm ; Room Number – C\4\45

Level/year at which this course is

offered

Level 7, 1st semester, 1435/1436

Pre-requisites for this course

(if any)

Medicinal Chemistry 1 (PCH 321)

Co-requisites for this course

(if any)

Organic Chemistry, Bio-chemistry, Analytical Chemistry and

Human Physiology.

Location if not on main campus Abha, KKU Main campus, Greger (Boys)

Total Number of Teaching Weeks 15 weeks

Total Number of Lectures Theory 30 Hours

Total Number of Practical Hours 60 Hours


COURSE DESCRIPTION

This course is designed to provide the knowledge to the students on physiochemical properties of therapeutic

agents such as cardiovascular drugs, Diuretic agents, Antihistamines, Gastrointestinal drug, Non-steroidal Anti-

inflammatory agents, Insulin and oral – hypo-glycemic agents and Opioid analgesics. This course also educates

students on the nomenclature, structure, chemistry and structure activity relationship of the above mentioned

therapeutic agents.

THE MAIN LEARNING OUTCOMES FOR STUDENTS ENROLLED IN THE COURSE

Summary of the main learning outcomes for students enrolled in the course.

After completing this course, students should be conversant with:

The physicochemical properties of the therapeutic agents and correlate physical and chemical properties of

drugs to their mechanism of action

Students should be able to describe basic structural features of drugs

Students can understand and be able to predict metabolic pathways of particular drugs

Structural modifications of drugs and their importance to increase the potency of the drug

They should be familiar with particular drug groups, structure-activity relationship and typical

representative examples used.

Prediction of the underlying mechanism of action on structural and molecular basis.

Exhibiting competence with respect to the method of synthesis and analysis of drugs in pure form and

pharmaceutical dosage forms

Critical awarness of Medicinal Chemistry and acquiring eligibility to do Medicinal Chemistry III course in

our college.


TEXT BOOK FOR REFERENCE

SCHEDULE OF ASSESSMENT TASKS

1) Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical Chemistry. 12th

Edition.

2) Foye’s “Principles of Medicinal Chemistry, Fifth Edition,” By David A. Williams and

Thomas L. Lemke, Lippincott Williams & Wilkins Publishers, New York, 2002.

3) Burger's Medicinal Chemistry and Drug Discovery 6th Ed (Vol. 1-6); Donald J. Abraham;

ISBN 0-471-27401-1; John Wiley & Sons, Inc; 2003


SCHEDULE OF ASSESSMENT TASKS

Examination protocol

QUIZ EXAM

It will have 10 written questions for 05 marks

Topics for Quiz-I

Date for Quiz Examinations will be announced through Black Board as per the agreement with

group leader

MID-TERM EXAM

24 MCQs 24 Marks 3 Short Answers out of 5 06 Marks Total 30 Marks

Topics for Mid-term exam

FOR MID TERM EXAMINATION, DATE, TIME AND PLACE OF EXAMINATION WILL BE INFORMED BY

ACADEMIC OFFICE.

Quiz exam 05 Marks Mid Term Theory Exam 30 Marks

E- Assignments 05 Marks

Mid Term practical Exam 10 Marks

Final practical Exam 10 Marks

Final Exam 40 Marks

Total 100 Marks

1. Cardiovascular system

MIDTERM EXAMINATION SYLLABUS INCLUDES TOPICS COVERED IN ANY FIVE WEEKS OF

THE TEACHING SCHEDULE


Assignments through E-Learning Activity

It will be given individually to the students from the topics of the course to do some online activities in

the black board. It will carry 05 marks

END SEMSTER EXAM

Final exam will consist of 60 multiple choice questions for 40 marks.

The mcqs will be from the topics covered from 6th teaching week onwards. FOR END SEMESTER EXAMINATION, DATE, TIME AND PLACE OF

EXAMINATION WILL BE INFORMED BY ACADEMIC OFFICE


TEACHING SCHEDULE FOR MEDICINAL CHEMISTRY-2-PCH- 422 THEORY

Theoretical Topics to be Covered

Week

No.

Topics Day and Date Instructor

1

1. CARDIOVASCULAR DRUGS:

1.1. CARDIOTONICS:

1.1.1. Cardiac Glycosides:

Chemistry of cardiac glycosides

Chemical stability of cardiac glycosides

Mode of action (MOA)

Toxicity

Structure Activity Relationship (SAR)

1.1.2. Non-steroidal cardiotonic agents:

Chemical structure, side effects and MOA of inamrinone and

milrinone

18-09-2016/

Sunday

2 credit hour

Dr. Kumar

Venkatesan

2 1.2. ANTI-ANGINAL DRUGS:

1.2.1.Organic Nitrates:

Formulation difficulties

Classification: Rapid and Slow acting formulations

Synthesis of iso-sorbide -dinitrate

Assay of nitrates

SAR

1.2.2. Calcium Channel Blockers:

1.2.2.1 1,4-dihydropyridines: Synthesis, nomenclature,

assay and SAR of some selected drugs.

1.2.2.2. Phenylalkylamines:Verapamil; MOA,

metabolism and synthesis.

1.2.2.3. Benzothiazepines:Diltiazem;

MOA, uses and nomenclature.

1.2.2.4. Diaminopropanol ethers: Bepridil; MOA.

25-09-2016/

Sunday

2 credit hour

Dr. Kumar

Venkatesan

3

1.3 ANTI-HYPERLIPIDIMIC DRUGS:

1.3.1. Bile acid binding resins: Cholestyramine

2-10-2016

Dr. Kumar


1.3.2. HMG-CoA reductase inhibitors: Structural features and

SAR of some selected drugs.

1.3.3. Fibrates: Structural features, MOA, synthesis, assay and SAR of some

selected drugs.

Sunday

2 credit hour

Venkatesan

4 1.4 ANTI-THROMBOTICS:

1.4.1 Oral anticoagulants:

Warfarin

Indanediones

1.4.2 Parentral anticoagulants:

Heparin

Low molecular weight heparins

9-10-2016/

Sunday

2 credit hour

Dr. Kumar

Venkatesan

5 1.5 ANTI-HYPERTENSIVE DRUGS:

Classification of antihypertensive drugs

The renin- angiotensin system

1.5.1. Angiotensin-Converting Enzyme Inhibitors:

1.5.1.1. Sulfhydryl-Containing Inhibitors:Captopril

1.5.1.2. Dicarboxylate-Containing Inhibitors: Enalapril,

Enalaprilat

1.5.1.3 Phosphonate-Containing Inhibitors:Fosinopril

1.5.2 Angiotensin Receptor Antagonists:

Losartan

Valsartan

1.5.3 Direct Vasodilators:

1.5.3.1.Calcium Channel Blockers

1.53.2.Potassium Channel Openers:

Diazoxide

Minoxidil

1.5.3.3.Other Vasodilators:

Hydralazine

Sodium nitroprusside

16-10-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan

6 2. Diuretics

2.1. Carbonic anhydrase inhibitors:

2.2.2 Loop diuretics:

5-Sulfamoyl-2- and -3-aminobenzoic acid derivatives: Furosemide,

Bumetanide. SAR and synthesis.

Phenoxyacetic acid derivatives: Ethacrynic acid. Uses, SAR and

synthesis.

23-10-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan


7 2.2.3. Thiazide and thiazide like diuretics: SAR, synthesis

and assay of selected drugs.

2.2.4. Potassium sparing diuretics:

Classification

Properties and uses

2.4.1. Aldosterone antagonists: Uses, adverse effects

and metabolism.

2.4.2 2,4,7 triamino-6-arylpteridines:

Triamterene

Amiloride hydrochloride

2.2.5.Osmotic diuretics:

30-10-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan

8 3. ANTIHISTAMINIC DRUGS: 3.1 Histamine and its receptors

3.2 Therapeutic uses of anti-histamines

3.3 Classification of Anti-histamines

3.3.1 First generation H1 anti-histamines

Alkylamines

Aminoalkylethers - SAR and Synthesis

Ethylenediamines

Propylamines: SAR and Synthesis

Piperazine derivatives

3.3.2 Second generation H1 anti-histamines:

Terfinadine

Astemizole

Loratadine

Cetrizine

3.4. Histamine release inhibitors: Cromolyn sodium

6-11-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan

9 4. GASTRO-INTESTINAL DRUGS:

4.1 Classification

4.2. Inorganic antacids:

Aluminum salts

Calcium carbonate

Magnesium salts

Bismuth salts

Simethicone

4.3. H2-receptor antagonists:

20-11-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan


First generation H2-receptor antagonists

Second generation H2-receptor antagonists

Third generation H2-receptor antagonists

4.4. Proton pump inhibitors:

Acid-catalyzed activation of omeprazole

SAR of proton pump inhibitors

10 5. NON-STEROIDAL ANTI-INFLAMMATORY DRUGS

MOA and Classification of NSAIDs

5.1.Salycilates:

Aspirin

Salycilates modified at the carboxyl group

Synthesis of diflunisal

SAR of salycilates

Assay

Purity of Aspirin

5.2.2 Aminophenol Derivatives:

Paracetamol; Identity test, assay and metabolism.

27-11-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan

11 5.3. N-arylanthranilic acids:

Mefenamic acid

Flufenamic acid

Meclofenamic acid

SAR

Synthesis of flufenamic acid

5.4. Arylacetic acids:

Indomethacin

Sulindac

Diclofenac

Tolmetin

SAR

Synthesis of Indomethacin

5.5. Arylpropionic acids:

Ibuprofen

Ketoprofen

Naproxen

Nabumetone

Synthesis of ibuprofen

Assay

4-12-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan


SAR of profens

12 5.6.Oxicams:

Pyroxicam

Tenoxicam

Meloxicam

Synthesis of pyroxicam

SAR of oxicams

5.7.Selective COX 2 Inhibitors:

7.7.1. Sulides

7.7.2. Tricyclics: Rofecoxib, Celecoxib.

Agents used for treatment of gout

Natraceuticals for osteoarthritis

11-12-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan

13

6. INSULIN AND ORAL HYPOGLYCEMIC AGENTS:

6.1 Diabetes - Introduction:

Types of diabetes

Complications of diabetes

Signs and symptoms of diabetes

Diagnosis of diabetes

6.2. Insulin:

Role of insulin

Chemistry of insulin

Dosage forms

Chemical stability

Insulin analogues and SAR

6.3. Oral hypoglycemics:

Sulfonylureas - SAR and MOA

Classification of Sulfonylureas - First, Second and Third

generation drugs

Synthesis and analysis of sulfonylureas

6.4. Thiazolidinediones: MOA

6.5. α-glucosidase inhibitors: MOA

6. 6. Biguanides: MOA

18-12-2016

Sunday

2 credit hour

Dr. Kumar

Venkatesan

14 7. OPIOID ANALGESICS:

Opium alkaloids

Morphine

Structure of morphine

SAR of morphine

25-12-2016

Sunday

Dr. Kumar

Venkatesan


Steriochemistry of morphine

Essential requirements for activity

Morphine receptors

2 credit hour

15 Morphine analogues:

o 1.1.Variation of substituents

o 1.2.Drug extension

o 1.3. Rigidification

o 1.4. Simplification:

Removing ring E

Removing ring D

Removing rings C & D

Removing rings B, C & D

Removing rings B,C, D & E

Synthesis of meperidine

Non-opoid analgesics: Nefopam, Tramadol

Endogenous opoids: SAR.

Antitussive agents

01-01-2017

Sunday

2 credit hour

Dr. Kumar

Venkatesan


TEACHING SCHEDULE FOR MEDICINAL CHEMISTRY-2-PCH- 422 PRACTICAL

Batch-A, Section 97, Wednesday, 01.00–03.00 PM; Lab No C/4/45

Week Date Topic Faculty Name

1 21-9-2016 Assay of Ibuprofen tablets Dr. Kumar Venkatesan &

Dr. Vel

2 28-9-2016 Assay of Captopril tablets “

3 05-10-2016 Assay of Povidone iodine topical solution “

4 12-10-2016 Assay of Sulfanilamide “

5 19-10-2016 Assay of Aspirin tablets “

6 26-10-2016 Assay of Ascorbic acid tablets “

7 02-11-2016 Revision “

8 09-11-2016 Practical Examination – I “

9 23-11-2016 Assay of Furosemide tablets “

10 30-11-2016 Assay of Propranolol tablets “

11 07-12-2016 Assay of Paracetamol tablets “


13 21-12-2016 Assay of Metoclopramide tablets “

14 28-12-2016 Revision “

15 04-01-2017 Practical Examination – II “


TEACHING SCHEDULE FOR MEDICINAL CHEMISTRY-2-PCH- 422 PRACTICAL

Batch-B, Section 98, Thursday, 01.00–03.00 PM; Lab No C/4/45

Week Date Topic Faculty Name

1 22-9-2016 Assay of Ibuprofen tablets Dr. Kumar Venkatesan &

Dr. Vel

2 29-9-2016 Assay of Captopril tablets ‘’

3 06-10-2016 Assay of Povidone iodine topical solution ‘’

4 13-10-2016 Assay of Sulfanilamide “


6 27-10-2016 Assay of Ascorbic acid tablets “

7 03-11-2016 Revision “

8 10-11-2016 Practical Examination – I “

9 24-11-2016 Assay of Furosemide tablets “

10 01-12-2016 Assay of Propranolol tablets “

11 08-12-2016 Assay of Paracetamol tablets “


13 22-12-2016 Assay of Metoclopramide tablets “

14 29-12-2016 Revision “

15 05-01-2017 Practical Examination - II “

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