Medicinal Chemistry III Module Overview B. Pharm., Semester-1 Course Code: 0510411, Session: 2016-2017 Facilitators and Module Coordinators DR. PRAN KISHORE DEB DR. BILAL AL-JAIDI Assistant Professor Faculty of Pharmacy, Philadelphia University, Jordan

Method of Delivery Method of Delivery No. of Activities Lectures 40 Workshops/Tutorials 05 Online Quiz (Kahoot) 15

Lecture Topics No. of Lectures Anticancer agents Alkylating Agents Heavy metal compounds (Metallating Agents) Anti-metabolites and Antibiotics Plant Extracts Topoisomerase inhibitors Combination of chemotherapy with other treatments 15 Diuretics Carbonic Anhydrase Inhibitors (CAIs) Loop Diuretics Thiazide and Thiazide-like Diuretics Potassium-sparing diuretics Osmotic diuretics 06 Respiratory drug development Design and Development of β2- Agonists and Treatment of Asthma 03 Cardiovascular drug development Development of β-blockers Calcium channel blockers Angiotensin converting enzyme inhibitors (ACE inhibitors) Angiotensin II receptor antagonists Direct acting vasodilator 14 Gastric drug development Development of Proton Pump Inhibitors 02 QUIZ-1 QUIZ-2 QUIZ-3

Class aims, objectives and rationale The class relates the structure and function of various proteins, receptors, enzymes and nucleic acids to drug discovery and action and provides a broad overview of the drug discovery and design process. There is particular emphasis on the factors (potency and efficacy, pharmacology and ADMET) that influences structure-activity relationships (SAR) as well as guide the development of small molecules into drug candidates and ultimately into drugs. Case examples from different therapeutic areas such as anti-cancer, cardiovascular, respiratory, diuretics and anti-ulcer agents are used to contextualise this process.

Learning outcomes: Upon the completion of this class, the student will be able to: Explain how protein (receptor, enzymes) and DNA structure relates to function with respect to their role as targets for drug discovery. Describe how active site topology controls specific catalytic processes that require regulation in different therapeutic scenarios. Outline how multidisciplinary scientific considerations during the lead optimisation process combine to produce a successful drug. Explain how knowledge of physicochemical properties in drug development can address problems encountered with formulation, administration, absorption and elimination. Describe how the requirements of drug development vary depending upon the specific target and the therapeutic area. Understand how previous drugs have been successfully developed using case studies that address varied administrative routes within a range of therapeutic areas (for example: anti-cancer agents, cardiovascular; respiratory; diuretics). Show how structural modifications of drugs within these therapeutic areas can be used to alter their pharmacodynamics and pharmacokinetics and overcome other issues (e.g. toxicity, prodrug design).

Assessment Methods Formative Assessment (Practice only, Kahoot Quiz & Tutorials) Summative Assessment (Marks included) Summative Assessment Type questions Duration Marks First Exam MCQs, Fill up the blanks, SAQs 1 hr 20 Second Exam Quizzes (3) Total 3 quizzes will be conducted. Average of the three quizzes will be considered 10 min Final Exam MCQs, SAQs, Fill up the blanks, True-False 2 hrs 40 Total 100

Recommended Books An introduction to Medicinal Chemistry by Graham L. Patrick. Fourth edition, Oxford, 2009. Wilson and Griswold’s Text Book of Organic Medicinal and Pharmaceutical Chemistry by John M. Beale, Jr. and John H. Black, Twelfth edition, Lippincott Williams and Wilkings 2011. Foye’s principle of medicinal chemistry by David H. Williams, Thomas L. Leuke, Williams O. Foye. Lippincot William and Wilkins. Seventh edition, 2012, ISBN.

Good Luck ……..