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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.

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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
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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

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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 4
th

edition (2009) Oxford University press , Oxford , UK .
3- William O. Foye Principle of Medicinal Chemistry, 6
th
edition
(2008), Lipincott Williams & Wilkins, London.
4- Wilson and Gisvolds Textbook of Organic, Medicinal and
Pharmaceutical Chemistry 10
th
edition (1998), Lippencott
Raven Publishers, Philadelphia, New York.
5- Andrejus Korolkovas Essentials of Medicinal Chemistry 2
nd

edition 1988, Wiley-interscience Publication, New York, USA.
c- (Recommended books):
1- Povl Krogsgaard - Larsen Textbook of Drug Design and Discovery
4
th
edition (2010), CRC Press, Raton, Fl, USA.
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2- Donald Cairns Essentials of Pharmaceutical Chemistry 3
rd
edition ,
(2008) Pharmaceutical press , London .
3- M. E. Wolff Burgers Medicinal Chemistry and Drug Discovery 5
th

edition (1997), Wiley-interscience Publication, New York.
4-A. Gennaro (Editor), Remingtons pharmaceutical Sciences, 21
th

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.
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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 1
st

Introduction,
Drug design and drug
metabolism
d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a6
a2, a6,a11
2
nd

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

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

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

Drug design and drug
metabolism
(Tutorial)
d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 6
th

Physicochemical
properties
(Drug design)
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d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 7
th

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

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

NSAIDs
(synthesis)
10
th

Midterm Exam
d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 11
th

NSAIDs
(Tutorial)
d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 12
th

PGs + Pharmaceutical
necessities
(Synthesis)
d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 13
th

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

Diagnostic agents +
Diuritics
(Synthesis)
d9,d12,d13 c7, c9, c11 b3, b4, b7, b11 a2, a6,a11 15
th

Diuritics
(Tutorial)


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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.
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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 H
2
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



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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)
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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 4
th
edition (2009) Oxford University press , Oxford , UK .
c) William O. Foye Principle of Medicinal Chemistry, 6
th
edition
(2008), Lipincott Williams & Wilkins, London.
d) Wilson and Gisvolds Textbook of Organic, Medicinal and
Pharmaceutical Chemistry 10
th
edition (1998), Lippencott
Raven Publishers, Philadelphia, New York.
e) Andrejus Korolkovas Essentials of Medicinal Chemistry 2
nd

edition 1988, Wiley-interscience Publication, New York, USA.
a) (Recommended books):
a) Povl Krogsgaard - Larsen Textbook of Drug Design and
Discovery 4
th
edition (2010), CRC Press, Raton, Fl, USA.
b) Donald Cairns Essentials of Pharmaceutical Chemistry 3
rd
edition , (2008) Pharmaceutical press , London .
c) M. E. Wolff Burgers Medicinal Chemistry and Drug
Discovery 5
th
edition (1997), Wiley-interscience Publication,
New York.
d) A. Gennaro (Editor), Remingtons pharmaceutical Sciences,
21
th
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
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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
















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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, a11 1
st

-lactam antibiotics
( Introduction)
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 2
nd

-lactams, tetracyclines,
chloramphenicol,
aminoglycosides
(limit test)
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 3
rd

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

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

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

GIT
(Analysis)
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 7
th

GIT + Antineoplastics
alkylating agent
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(Discussion of report)
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 8
th

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

Antimetabolites
(Discussion of report)
10
th

Midterm Exam
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 11
th

Antifungal, + Antiviral
(Analysis)
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 12
th

Anthelmentics + Anti TB
(Discussion of report)
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 13
th

Antiprotozoal
(Analysis)
d1,d8, d9,d12,d13 c7,c 9,c11 b3,b4,b7,b11 a2, a6, a11 14
th

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)









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