Undergraduate courses information activities - aun.edu.eg · 2-Practical Medicinal Chemistry (Part 1) b- Essential Books (Text Books): 1- J.L.Mc.Guire “Pharmaceuticals”, Classes,

Undergraduate courses information & activities

Medicinal Chemistry 2010 Page 1

Medicinal Chemistry 1

1-Basic Information

Title: Medicinal Chemistry 1 Code: PHC - 415

Level: Third year (1 st Semester)

Department: Medicinal Chemistry

Unit: Lecture: 2(2hrs) Tutorial/ Practical:1(3hrs) Total: 3(5 hrs)

2- Aims of Course

1- Provide the basic knowledge of medicinal chemistry, through

identification of the chemistry of different drug classes including analgesics

and anti-inflammatory, diuretics, diagnostic agents pharmaceutical

necessities, drug metabolism, drug design and physicochemical parameters.

2- Acquire the knowledge about drug synthesis, analysis, mechanism of

action and SAR.

3- Provide the basics of the concept of drug design and prodrug

approaches as well as physicochemical parameters affecting drug action,

absorption and bioavailability.

3- Intended Learning Outcomes of Course(ILOs)

a- Knowledge and Understanding:

a 2-Basic understanding of physicochemical properties of drugs including

electronic, lipophilic, steric parameters in relation to synthetic,

biotechnology and radiolabled products.

a 6- Appropriate knowledge concerning chemistry of medicinal agents,

their synthesis, isolation, identification by spectral techniques as well as

structural activity relation ship (SAR) and drug design

a11- Activity and toxic profile of various drugs deduced from structure,

and biotransformation processes.



b- Intellectual Skills:

b3- Predict the methods of synthesis and properties of medicinal agents

and their relation to molecular structure.

b4- Apply spectral data for identification of raw materials as well as

pharmaceutical compounds.

b7- Integrate information and propose approaches for monitoring and

design of medicinal agents of different sources.

b11- Select and assess appropriate methods of extraction, isolation,

purification, identification of medicines from synthetic origin.

c- Professional and practical Skills:

c7- Handle properly chemicals in the lab and be aware of the rules of

good laboratory practice(GLP).

c9- Synthesize, isolate and identify drug molecules.

c11- Conduct research studies and analyze results.

d- General and Transferable Skills:

d9- Work effectively in a team and present results in written and oral

forms.

d12- Manage the time effectively in laboratory and home work.

d13- Demonstrate critical thinking, problem solving and decision making

abilities through tutorial classes.

Course Contents

Topic Total hours Lecture Tutorial / Practical

Introduction 4 1 3

Physicochemical properties

of drug molecules

8 2 6

Analgesics and anti-

inflammatory

14 8 6



Prostaglandins 1 1 --

Diuretics 6 3 3

Diagnostic agents 6 3 3

Pharmaceutical necessities 4 1 3

Drug design and drug

metabolism

24 9 15

4- Teaching and Learning Methods

4.1- Lectures.

4.2- Practical training (Laboratory).

4.3-Tutorials and class activity.

5- Teaching and learning methods for disables

5.1- Office hours.

5.2- Tutorials.

5.3- Revision of practical part.

6- Student Assessment

a- Student Assessment methods

6.1-Written exam to assess ILOs: a, b, c

6.2- Oral exam to assess ILOs: a, b, c and d

6.3- Practical exam to assess ILOs: a, b, c and d

6.4-Tutorial classes to assess ILOs: a, b and d

b- Student Assessment Schedule

No. Assessment week

1. Practical exam every week

2. Mid-Term exam 13 th

3. Final written exam 17 th

4. Oral exam 17 th



c- Weighting of Assessments

No. Exam. Mark %

1. Mid-Term Examination 15 10

2. Final-Term Examination 70 46.7

3. Oral Examination 20 13.3

4. Practical Examination 45 30

5. Semester Work - -

6- Other types of assessment - -

Total 150 100%

7- List of References

a-Course Notes:

1- Lectures in Medicinal Chemistry (Part 1)

2- Practical Medicinal Chemistry (Part 1)

b- Essential Books (Text Books):

1- J.L.Mc.Guire “Pharmaceuticals”, Classes, Therapeutic agents,

Areas of Application, 2000, Wiley-VCH Verlag GmbH, Weinheim.

2- Graham Patrick “An Introduction to Medicinal Chemistry” 4th

edition (2009) Oxford University press , Oxford , UK .

3- William O. Foye “ Principle of Medicinal Chemistry, 6th edition

(2008), Lipincott Williams & Wilkins, London.

4- Wilson and Gisvolds “Textbook of Organic, Medicinal and

Pharmaceutical Chemistry” 10th edition (1998), Lippencott –

Raven Publishers, Philadelphia, New York.

5- Andrejus Korolkovas “Essentials of Medicinal Chemistry” 2nd

edition 1988, Wiley-interscience Publication, New York, USA.

c- (Recommended books):

1- Povl Krogsgaard - Larsen “Textbook of Drug Design and Discovery”

4th edition (2010), CRC Press, Raton, Fl, USA.



2- Donald Cairns “Essentials of Pharmaceutical Chemistry 3rd edition ,

(2008) Pharmaceutical press , London .

3- M. E. Wolff Burger’s Medicinal Chemistry and Drug Discovery” 5th

edition (1997), Wiley-interscience Publication, New York.

4-A. Gennaro (Editor), Remington’s pharmaceutical Sciences, 21th

edition (2006), Lippincott Williams & Wilkins, Maryland, USA.

5- Egyptian Pharmacopoeia (1984)

6- United State Pharmacopoeia (2007)

7- British Pharmacopoeia (2009)

8- European Pharmacopoeia Vol. 2 (2008)

d- (Periodicals, Web Sites…. etc)

http://depts.washington.edu/medchem/420temp.html

http://depts.washington.edu/medchem/courses.html

http://www.personal.umich.edu/-rww/

http://www.nottingham.ac.uk/pharmacy/undergraduate/modu.html

http://www.pharmacy.purdute.edu/-mcm408/sylabus.pdf

http://www.rci.rutgers.edu/-layla/medchem/AMCL.htm

http://www.neurosci.pharm.utoledo.edu/MBC3320.html

8- Facilities Required for Teaching and Learning

Computer modeling and computational chemistry programs.



University Assiut.

Course Title Medicinal chemistry1

Faculty Pharmacy Course Cod. PHC - 415 Department Medicinal Chemistry.

Matrix of the Intended Learning Outcomes (ILOs) of the Course

General and

Transferable Skills Professional and Piratical Skills

Intellectual Skills

Knowledge and Understanding

Week Topic

d9,d12,d13 c7, c11 b4, b11 a6 1st Introduction, Drug design and drug metabolism

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a6 a2, a6,a11

2nd Drug design and drug metabolism (Drug design)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 3rd Drug design and drug metabolism (Tutorial)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 4th Drug design and drug metabolism (Drug design)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 5th Drug design and drug metabolism (Tutorial)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 6th Physicochemical properties (Drug design)



d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 7th NSAIDs (synthesis)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 8th NSAIDs (Tutorial)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 9th NSAIDs (synthesis)

10th Midterm Exam

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 11th NSAIDs (Tutorial)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 12th PGs + Pharmaceutical necessities (Synthesis)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 13th Diagnostic agents (Tutorial)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 14th Diagnostic agents + Diuritics (Synthesis)

d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 15 th Diuritics (Tutorial)


Medicinal Chemistry Page 8

Medicinal Chemistry 2 1-Basic Information Title: Medicinal Chemistry 2 Code: PHC - 457 Level: Third year (2 nd Semester) Department: Medicinal Chemistry Unit: Lecture:2(2 hrs) Tutorial/ Practical:1(3hrs) Total: 3(5 hrs) 2- Aims of Course 1-The course aims to provide the pharmacy students the basic knowledge in the domain of Medicinal chemistry through identification of the chemistry of different drug groups including chemotherapeutic agents as antibiotics, antineoplastics, antiviral, antiprotozoal, antifungals, anti-tubercular , sulfonamides, and anthelmintics 2- Provide the Knowledge about drug synthesis, drug analysis, drug bioreactivity, SAR, and drug metabolism. 3- Afford the basics of computer aided drug design, starting from a known lead or using a known receptor structure. 4- Provide the knowledge about different sources of inorganic impurities and related substances and their evaluation in raw materials using different pharmacopoeias. 3- Intended Learning Outcomes of Course(ILOs) a- Knowledge and Understanding:

a 2-Basic understanding of physicochemical properties of drugs including electronic, lipophilic, steric parameters in relation to synthetic, and biotechnology. a 6- Appropriate knowledge concerning chemistry of medicinal agents, their isolation, synthesis, purification, identification and application of different analytical techniques for their estimation in dosage forms as well as structural activity relationship (SAR) and drug design a11- Activity and toxic profile of various drugs deduced from structure, and metabolism. b- Intellectual Skills: b3- Predict the methods of synthesis and properties of medicinal agents and their relation to molecular structure by applying the principles of bio-informatics and computer aided tools in drug design.



b4- Apply qualitative and quantitative analytical methods for identification of impurities, quality control and assay of raw materials as well as pharmaceutical preparations. b7- Integrate information and propose approaches for monitoring and design of medicinal agents of different sources. b11- Select and asses appropriate methods of extraction, isolation, purification, identification, standardization of medicines from synthetic origin. c- Professional and practical Skills: c7- Handle properly chemicals in the lab and be aware of the rules of good laboratory practice(GLP). c9- Synthesize, isolate, identify, standardize drugs in formulations c11- Conduct research studies and analyze results. d- General and Transferable Skills: d1- Apply information technology skills, including word processing, database use, archiving data and information retrieval through online computer searches, and internet communication. d8- Acquire independent study skills and problem solving in groups. d9- Work effectively in a team and present results in written and oral forms. d12- Manage the time effectively in laboratory and home work. d13- Demonstrate critical thinking, problem solving and decision making abilities through tutorial classes. Course Contents

Topic Total hours Lecture Tutorial / Practical GIT 14 5 9 Histamine H2 antagonists 5 2 3 Antibiotics 8 6 3 Antineoplastic Antiviral 15 6 9 Antiprotozoan, Anthelmintics 10 4 6

Anti-tubercular, Antifungal 8 2 6 Sulfonamides 5 2 3 General anti bacterials 4 1 3



4- Teaching and Learning Methods 4.1- Lectures. 4.2- Practical training (Laboratory). 4.3-Tutorials and class activity. 4.4- Internet search and discussion

5- Teaching and learning methods for disables 5.1- Office hours. 5.2- Tutorials. 5.3- Revision of practical part. 6- Student Assessment a- Student Assessment methods

6.1-Written exam to assess ILOs: a, b, c 6.2- Oral exam to assess ILOs: a, b, and d 6.3- Practical exam to assess ILOs: a, b, c and d 6.4-Tutorial classes to assess ILOs: a, b and d

b- Student Assessment Schedule

No. Assessment week 1. Practical exam every week 2. Mid-Term exam 10 th 3. Oral exam 17 th 4. Final written exam 17 th

c- Weighting of Assessments No. Exam. Mark % 1. Mid-Term Examination 15 10 2. Final-Term Examination 70 46.7 3. Oral Examination 20 13.3 4. Practical Examination 45 30 5. Semester Work - - 6- Other types of assessment - - Total 150 100%

7- List of References

a-Course Notes: 1- Lectures in Medicinal Chemistry (Part 2)



2- Practical Pharmaceutical Chemistry (2)

b- Essential Books (Text Books): a) J.L.Mc.Guire “Pharmaceuticals”, Classes, Therapeutic agents,

Areas of Application, 2000, Wiley-VCH Verlag GmbH, Weinheim.

b) Graham Patrick “An Introduction to Medicinal Chemistry” 4th

edition (2009) Oxford University press , Oxford , UK . c) William O. Foye “ Principle of Medicinal Chemistry, 6th edition

(2008), Lipincott Williams & Wilkins, London. d) Wilson and Gisvolds “Textbook of Organic, Medicinal and

Pharmaceutical Chemistry” 10th edition (1998), Lippencott – Raven Publishers, Philadelphia, New York.

e) Andrejus Korolkovas “Essentials of Medicinal Chemistry” 2nd edition 1988, Wiley-interscience Publication, New York, USA.

a) (Recommended books): a) Povl Krogsgaard - Larsen “Textbook of Drug Design and

Discovery” 4th edition (2010), CRC Press, Raton, Fl, USA. b) Donald Cairns “Essentials of Pharmaceutical Chemistry 3rd

edition , (2008) Pharmaceutical press , London . c) M. E. Wolff Burger’s Medicinal Chemistry and Drug

Discovery” 5th edition (1997), Wiley-interscience Publication, New York.

d) A. Gennaro (Editor), Remington’s pharmaceutical Sciences, 21th edition (2006), Lippincott Williams & Wilkins, Maryland, USA.

e) Egyptian Pharmacopoeia (1984) f) United State Pharmacopoeia (2007) g) British Pharmacopoeia (2009) h) European Pharmacopoeia Vol. 2 (2008) b- Periodicals, Web Sites…. etc) J. Pharm. Pharmacol. 53,841-848 (2001)

http://depts.washington.edu/medchem/420temp.html http://depts.washington.edu/medchem/courses.html http://www.personal.umich.edu/-rww/ http://www.nottingham.ac.uk/pharmacy/undergraduate/modu.html http://www.pharmacy.purdute.edu/-mcm408/sylabus.pdf



http://www.rci.rutgers.edu/-layla/medchem/AMCL.htm

http://www.neurosci.pharm.utoledo.edu/MBC3320.html

8- Facilities Required for Teaching and Learning Computer modeling and computational chemistry programs: Molecular Operating environment (MOE) Program



University Assiut.

Course Title Midicinal Chemistry 2

Faculty Pharmacy Course Cod. PHC-457 Department Medicinal Chemistry.

Matrix of the Intended Learning Outcomes (ILOs) of the Course

General and

Transferable Skills Professional and Piratical Skills

Intellectual Skills

Knowledge and Understanding

Week Topic

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a111st β-lactam antibiotics ( Introduction)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 2nd β-lactams, tetracyclines, chloramphenicol, aminoglycosides (limit test)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 3rd Macrolides, quinolones, classification (limit test)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 4th Antihistamines, (limit test)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 5th GIT (limit test)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 6th GIT (Analysis)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 7th GIT + Antineoplastics alkylating agent



(Discussion of report) d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 8th Antimetabolites, natural

products (Analysis)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 9th Antimetabolites (Discussion of report)

10th Midterm Exam

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 11th Antifungal, + Antiviral (Analysis)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 12th Anthelmentics + Anti TB (Discussion of report)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 13th Antiprotozoal (Analysis)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 14th Antimalarial (Discussion of report)

d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 15 th Sulfa Drugs + H2 Antagonist (Analysis)



Documents

Undergraduate courses information activities - aun.edu.eg · 2-Practical Medicinal Chemistry (Part 1) b- Essential Books (Text Books): 1- J.L.Mc.Guire “Pharmaceuticals”, Classes,