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An-Najah National University College of medicine and health sciences Department of Pharmacy Medicinal chemistry 1 (7303301) First semester 2013/2014 Course Description: The aim of this course is to introduce the basic concepts of medicinal chemistry. Study the physicochemical properties of the drugs and study their distribution, metabolism and excretion. The course will discuss specific drug classes by covering its chemistry, some synthesis, mechanism of action and its structural activity relationship (SAR). Course objectives: Recognize the relation between the drug chemical structure and its biological activity in the body. The importance of organic functional groups in determining the physicochemical properties of the drug. Understand the interactions drug-protein, drug-enzyme, and drug-receptor. How the body interacts and makes changes on the chemical structure of the drug. Introduce various classes of therapeutic agents with the emphasis on their structure activity relationship (SAR). Intended learning outcomes (ILOs): a. Knowledge and understanding: a.1 Recognise and identify drug receptor, drug enzyme, drug protein interactions a.2 Be familiar with the main classification of drugs a.3 Describe the physicochemical properties of drugs and its roll in drugs absorption to blood circulation and crossing of system barriers a.4 Identify The Henderson-Hasselbalch Equation in calculating the drug ionization and its effect on drug absorption a.5 Describe importance of water solubility of drug and relate it to its chemical structure. a.6 Define the biological factors that affect the drug metabolism a.7 Define the different phases of drug metabolism in the body (phase I and phase II) with their different chemical modifications. a.8 Describe the SAR of different types and classes of drugs b. Intellectual Skills: b.1 Differentiate between drug as an enzyme substrate and its action on a cell receptor b.2 Differentiate between ionisable and non ionisable drug functional group b.3 Recognise the hydrophilic and lipophilic properties of the drug chemical structure. b.4 Differentiate between the general chemical reaction involved in Phase I and Phase II drug metabolism. b.5 Recognise the medicinal action of chemical compounds according to their structure. c. Professional and practical skills: c.1 Be able to propose new drug chemical structure to modify drug activity c.2 Be able to resolve problems related to drug solubility and absorbtivity in mammalian system c.3 Be able propose chemical modifications to different types of drug formulations d. General and transferable skills: Search the internet database for current chemical modification of newly developed d.1 antibacterial, anti-infective drugs and Non-Steroidal Anti-Inflammatory drugs (NSAIDs) d.2 Independent learning through literature searching and presenting work. d.3 Appreciate team work in the seminar d.4 Work in a team d.5 Respect assisting personal. Course Outline: Topics Week/ hours Chapter I: Introduction to medicinal chemistry History of medicinal chemistry Drug Discovery General Classification of drugs 1.5hours Chapter II: Introduction of drug targets Cell structure Cell membrane Drug targets Intermolecular bonding forces 1.5hours Chapter III: Proteins as drug targets The building blocks of protein and their structure Protein function 1.5hours Chapter IV: Enzymes as drug targets Overall Process of Enzyme Catalysis Enzyme targets for useful medications 1.5hours Chapter V: Receptors as drug targets Receptor function Messenger binding Overall Process of Receptor/Messenger Interaction Design of Agonists Design of Antagonists 2hours Chapter VI: Review of important functional groups. Nitrogen Containing Functional Groups. Oxygen Containing Functional Groups Aromatic Hydrocarbons Heterocycles 5hours Chapter VII: Pharmacokinetic of drugs a. Drug absorption & distribution Ionisation of Drug Molecules Drug Partition coefficient Solubility of Drugs Distribution b. Drug metabolism & Excretion Biological factors affecting metabolism Pharmacological effect of metabolism on drugs Phase I metabolic reactions Phase II metabolic reaction or conjugation reaction excretion 10hours Chapter VIII: Anti-infective drugs: Desinfectants & antiseptics Antifungal Antiprotozoal Agents Anthelmintics Antimalarial 7hours Chapter IX: Antibacterial agent Antibacterial agents which act against cell metabolism Antibacterial agents which inhibit cell wall synthesis Antibacterial agents which act on the plasma membrane structure 9 hours Antibacterial agents which impair protein synthesis: translation Agents which act on nucleic acid: transcription and replication Chapter X: Antiviral agent Structure & life cycle of viruses Antiviral drugs used against DNA viruses Antiviral drugs acting against RNA viruses: HIV Antiviral drugs Agents for the treatment of influenza 5hours Chapter XI: Nonsteroidal Anti-inflammatory Drugs “NSAIDS” Classes of COX inhibitors The COX binding site The salicylates Fenemates p-Aminophenols Arylacetic acid derivatives Arylpropioanic acid derivatives Oxicams Miscellaneous Total hours 4hours 48 Text Books: - Foye's principles of medicinal chemistry, Williams DA and Lemke TL, Sixth edition. 2008, Lippincott Williams & Wilkins - An Introduction to Medicinal Chemistry by Graham L. Patrick, fifth edition.2013, Oxford University Press, USA; - Textbook of organic medicinal and pharmaceutical chemistry, by Wilson and Gisvold's, Eleventh edition. Lippincott Williams & Wilkins, 2011. Medicinal Chemistry Gareth Thomas, Second Edition ,Wiley, 2007. - Medicinal chemistry by Ashtush Kar- fourth edition. New Age International, 2007. - Grades: 1st Exam: 20%.....2/10/2013 “Wednesday” 2nd Exam: 20%.....11/11/2013 “Moneday” Quizes, participation & attendance: 10% Presentation: 10% Final Exam: 40%