Medicinal Chemistry 1

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1 Medicinal Chemistry 1 1-Basic Information Title: Medicinal Chemistry 1 Code: PHC 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. Medicinal Chemistry 2010 Page 1

2 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 Physicochemical properties of drug molecules Analgesics and antiinflammatory Medicinal Chemistry 2010 Page 2

3 Prostaglandins Diuretics Diagnostic agents Pharmaceutical necessities Drug design and drug metabolism 4- Teaching and Learning Methods 4.1- Lectures Practical training (Laboratory). 4.3-Tutorials and class activity. 5- Teaching and learning methods for disables 5.1- Office hours Tutorials 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 Medicinal Chemistry 2010 Page 3

4 c- Weighting of Assessments No. Exam. Mark % 1. Mid-Term Examination Final-Term Examination Oral Examination Practical Examination Semester Work Other types of assessment - - Total % 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. Medicinal Chemistry 2010 Page 4

5 2- Donald Cairns Essentials of Pharmaceutical Chemistry 3 rd edition, (2008) Pharmaceutical press, London. 3- M. E. Wolff Burger s Medicinal Chemistry and Drug Discovery 5 th edition (1997), Wiley-interscience Publication, New York. 4-A. Gennaro (Editor), Remington s 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) Facilities Required for Teaching and Learning Computer modeling and computational chemistry programs. Medicinal Chemistry 2010 Page 5

6 University Assiut. Course Title Medicinal chemistry1 Faculty Pharmacy Course Cod. PHC Department Medicinal Chemistry. Matrix of the Intended Learning Outcomes (ILOs) of the Course Topic Introduction, Drug design and drug metabolism Drug design and drug metabolism (Drug design) Drug design and drug metabolism (Tutorial) Drug design and drug metabolism (Drug design) Drug design and drug metabolism (Tutorial) Physicochemical properties (Drug design) Week 1 st 2 nd 3 rd 4 th 5 th 6 th Knowledge and Understanding a6 a6 Intellectual Skills b4, b11 Professional and Piratical Skills c7, c11 General and Transferable Skills Medicinal Chemistry 2010 Page 6

7 NSAIDs (synthesis) NSAIDs (Tutorial) NSAIDs (synthesis) Midterm Exam NSAIDs (Tutorial) PGs + Pharmaceutical necessities (Synthesis) Diagnostic agents (Tutorial) Diagnostic agents + Diuritics (Synthesis) Diuritics (Tutorial) 7 th 8 th 9 th 10 th 11 th 12 th 13 th 14 th 15 th Medicinal Chemistry 2010 Page 7

8 Medicinal Chemistry 2 1-Basic Information Title: Medicinal Chemistry 2 Code: PHC 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, antitubercular, 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 bioinformatics and computer aided tools in drug design. Medicinal Chemistry Page 8

9 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 Histamine H 2 antagonists Antibiotics Antineoplastic Antiviral Antiprotozoan, Anthelmintics Anti-tubercular, Antifungal Sulfonamides General anti bacterials Medicinal Chemistry Page 9

10 4- Teaching and Learning Methods 4.1- Lectures Practical training (Laboratory). 4.3-Tutorials and class activity Internet search and discussion 5- Teaching and learning methods for disables 5.1- Office hours Tutorials 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 Final-Term Examination Oral Examination Practical Examination Semester Work Other types of assessment - - Total % 7- List of References a-course Notes: 1- Lectures in Medicinal Chemistry (Part 2) Medicinal Chemistry Page 10

11 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 Burger s Medicinal Chemistry and Drug Discovery 5 th edition (1997), Wiley-interscience Publication, New York. d) A. Gennaro (Editor), Remington s 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, (2001) Medicinal Chemistry Page 11

12 Facilities Required for Teaching and Learning Computer modeling and computational chemistry programs: Molecular Operating environment (MOE) Program Medicinal Chemistry Page 12

13 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 Topic β-lactam antibiotics ( Introduction) β-lactams, tetracyclines, chloramphenicol, aminoglycosides (limit test) Macrolides, quinolones, classification (limit test) Antihistamines, (limit test) GIT (limit test) GIT (Analysis) GIT + Antineoplastics alkylating agent Week 1 st 2 nd 3 rd 4 th 5 th 6 th 7 th Knowledge and Understanding Intellectual Skills Professional and Piratical Skills General and Transferable Skills d1,d8, d1,d8, d1,d8, d1,d8, d1,d8, d1,d8, d1,d8, Medicinal Chemistry Page 13

14 (Discussion of report) Antimetabolites, natural products (Analysis) Antimetabolites (Discussion of report) Midterm Exam Antifungal, + Antiviral (Analysis) Anthelmentics + Anti TB (Discussion of report) Antiprotozoal (Analysis) Antimalarial (Discussion of report) Sulfa Drugs + H2 Antagonist (Analysis) 8 th 9 th 10 th 11 th 12 th 13 th 14 th 15 th d1,d8, d1,d8, d1,d8, d1,d8, d1,d8, d1,d8, d1,d8, Medicinal Chemistry Page 14

15 Medicinal Chemistry Page 15

Course Specification Medicinal Chemistry-1

Quality Assurance Unit Faculty of Pharmacy-Assiut University Course Specification Medicinal Chemistry-1 Programme(s) on which the course is given: B. Sc. (Pharmaceutical science) Major or Minor element