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1 Medicinal Chemistry 3 1-Basic Information Title: Medicinal Chemistry 3 Code: PHC-515 Level: Fourth year (1 st Semester) Department: Medicinal Chemistry Unit: Lecture:2(2hrs) Tutorial/ Practical:1(3 hrs) Total:3(5 hrs) 2- Aims of Course 1-The course aims to recognize the pharmacy students the basic knowledge in the domain of Medicinal chemistry through identification of the chemistry of different drug groups including adrenergic and cholinergic, central relaxant, neuromuscular blockers, antiparkinsonism, general anesthesia, sedative hypnotics, antipsychotics, antianxiety, CNS stimulant, cardiotonics, antihypertensive, vasodilator and anticoagulant. 2-Provide the students drug synthesis, drug analysis, drug bioreactivity, SAR, and drug metabolism. 3-Recognize the students drug design which concerned with the most of the methods known to discover a new drug entity whether it is mathematical or non-mathematical, computer aided or not, starting from a known lead or using a known receptor structure. 4- Provide the student the different intended learning outcomes of Med. Chem. 3 (ILOs) 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 relationships (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. b4- Apply qualitative and quantitative analytical methods for identification, quality control and assay of raw materials as well as pharmaceutical preparations. b7- Apply information and propose approaches for monitoring and design of medicinal agents of different sources. Medicinal Chemistry Page 1

2 b11- Select and assess appropriate methods of extraction, isolation, purification, identification and standardization 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- Isolate, synthesize, identify and 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, problems solving and decision making abilities through a tutorial classes. Course Contents Topic No. of hours Lecture Tutorial / Practical Adrenergics Cholinergics Central relaxant, Neuromuscular blockers, antiparkinsonism General anesthetics Sedative hypnotics Antianxiety + Antipsychotics CNS stimulants Cardiotonics Antihypertensives Vasodilator anticoagulants 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. Medicinal Chemistry Page 2

3 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: a)topics in Medicinal Chemistry (Part 3) b)practical Pharmaceutical Chemistry ( Part 3) 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), Lippencott, 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. Medicinal Chemistry Page 3

4 c- (Rcommended 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) d- (Periodicals, Web Sites. etc) Facilities Required for Teaching and Learning Computer modeling and computational chemistry programs. Molecular Operating environment (MOE) Program Medicinal Chemistry Page 4

5 University Assiut. Course Title Midicinal chemistry 3 Faculty Pharmacy Course Cod. PHC-515 Department Medicinal Chemistry. Matrix of the Intended Learning Outcomes (ILOs) of the Course Topic General anesthetics (Drug Analysis) Sedative, hypnotics (Tutorial) AntiPsychotics + Antianxiety (Drug Analysis) Anticonvulsants (Tutorial) CNS stimulants (Drug Analysis) Adrenargics Discussion of the report Adrenargics (Drug Analysis) Cholinergics Discussion of the report Week 1 st 2 nd 3 rd 4 th 5 th 6 th 7 th 8 th Knowledge and Understanding Intellectual Skills Professional and Piratical Skills General and Transferable Skills Medicinal Chemistry Page 19

6 Cholinergics (Drug Analysis) Periodical Exam Cholinergics Antiparkinsonism (Report Discussion) Antiparkinsonism Cardiotonic drugs (Drug Analysis) Vasodilators, antiarrythmics, (Report Discussion) antihypertensive drugs Coagulant and anticoagulant, antilipidemic drugs (Tutorial) 9 th 10 th 11 th 12 th 13 th 14 th, 15 th Medicinal Chemistry Page 20

7 Medicinal Chemistry 4 1-Basic Information Title: Medicinal Chemistry 4 Code: PHC- 557 Level: Fourth year (2 nd semester) Department: Medicinal Chemistry Unit: Lecture:2(2 hrs) Tutorial/ Practical:1(3 hrs) Total:3(5 hrs) 2- Aims of Course 1-The course aims to recognize the pharmacy students the basic knowledge in the domain of medicinal chemistry through identification of the chemistry of different drug groups including peptide hormones, oral hypoglycemic, antithyroids, steroidal hormones, vitamins and local anesthetics 2-Provide the students knowledge about drug synthesis, drug analysis, drug bioreactivity, SAR, and drug metabolism. 3-Recognize the students drug design which concerned with the most of the methods known to discover a new drug entity whether it is mathematical or non mathematical, computer aided or not, starting from a known lead or using a known receptor structure. 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. b4- Apply qualitative and quantitative analytical methods for identification, quality control and assay of raw materials as well as pharmaceutical preparations. b7- Apply 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, and standardization of medicines from synthetic origin. Professional and practical Skills: Medicinal Chemistry Page 21

8 c7- Handle properly chemicals in the lab and be aware of the rules of good laboratory practice(glp). c9- Synthesize, isolate and identify activity of drug molecules by computer programs. 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 a tutorial classes. Course Contents Topic Total hours Lecture Tutorial / Practical Pituitary and hypothalamic hormones Anterior, Posterior pituitary hormones, prostaglandine Pancreatic hormones Oral hypoglycemic, thyroid hormones Estrogen, antiestrogen Progestrone,antiprogestrone Testestrone, anabolic drugs Adreno, mineralo corticoid, Local anesthetics Water soluble, fat soluble vitamin Teaching and Learning Methods 4.1- Lectures Practical training (Laboratory). 4.3-Tutorials and class activity Discussion and internet search. 5- Teaching and learning methods for disables 5.1- Office hours Tutorials Revision of practical part. Medicinal Chemistry Page 22

9 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: a) Topics in Medicinal Chemistry (Part 4) b) Practical Medicinal Chemistry ((Part 4) b- Essential Books (Text Books): f) J.L.Mc.Guire Pharmaceuticals, Classes, Therapeutic agents, Areas of Application, 2000, Wiley-VCH Verlag GmbH, Weinheim. g) Graham Patrick An Introduction to Medicinal Chemistry 4 th edition (2009) Oxford University press, Oxford, UK. h) William O. Foye Principle of Medicinal Chemistry, 6 th edition (2008), Williams & Wilkins, London. i) Wilson and Gisvolds Textbook of Organic, Medicinal and Pharmaceutical Chemistry 10 th edition (1998), Lippencott Raven Publishers, Philadelphia, New York. j) 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 Page 23

10 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) (Periodicals, Web Sites. etc) Facilities Required for Teaching and Learning Computer modeling and computational chemistry programs. Medicinal Chemistry Page 24

11 University Assiut. Course Title Faculty Pharmacy Course Cod. PHC Department Medicinal Chemistry. Medicinal Chemistry 4 Matrix of the Intended Learning Outcomes (ILOs) of the Course Topic Pituitary, hypothalamic hormones ( Introduction) Anterior Pituitary hormones (Drug Design) Posterior Pituitary hormones (Drug Design) Pancreatic hormones (Drug Design) Oralhypoglycemic, (Drug Design) Thyroid hormones (Drug Design exam) Estrogen, antiestrogen (Synthesis) 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 Medicinal Chemistry Page 25

12 Progestrone,antiprogestrone (Tutorial) Testosterone, anabolic drugs (Synthesis) Periodical Exam Adrenocorticoids (Synthesis) Water soluble vitamins (Tutorial) Water soluble vitamins (Synthesis) Fat soluble vitamins (Tutorial) Local anesthetics (Synthesis exam) 8 th 9 th 10 th 11 th 12 th 13 h 14 th 15 th Medicinal Chemistry Page 26

13 Medicinal Chemistry Page 27

Medicinal Chemistry 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)