Educational offer - University of Padova

Syllabus

Prerequisites:	The student should have a preliminary knowledge in cell biology and physiology, and extensive knowledge of biochemistry. He/she must know well organic chemistry, able in recognizing the structures and nomenclature of organic structures and heterocycles. Knowledge of the English language is mandatory.
Target skills and knowledge:	The teaching is based on lectures in English, supplemented by lectures given by experts, if possible. At the end of the course the student will know the strategies of drug discoveryof small molecules with therapeutic activity, will know the molecular basis of the action of drugs, in particular regarding their interaction with biological targets of therapeutic relevance, and he/she will be able to discuss the principles underlying the discovery and development of drugs.
Examination methods:	Multiple choice test through Moodle platform (online, in presence)
Assessment criteria:	The exam at the end of course aims to test the student's ability to discuss in an autonomous and critical way on all aspects related to the rationale at the basis of the discovery and molecular activity of drugs.
Course unit contents:	The course focuses on the molecular basis of target-based drug discovery, with emphasis on the biological targets of therapeutic relevance for rational discovery & development of small molecules drugs. Topics covered through the course are: Principles governing drug-receptor interactions, molecular mechanism of drug-receptor recognition, stereochemistry. Discovery of Lead compounds, structure-activity relationships. Rational development of drugs: natural products and existing drugs as chemical scaffolds for the discovery and design of novel therapeutics, analog design, computer-aided rational design, peptidomimetics. Examples treated in details will be benzodiazepines, opioid analgesics, renin-angiotensin-aldosterone inhibitors, Histamine-2 antagonist, COX-inhibitors and kinase inhibitors. Particular attention will be devoted to the discovery and development of HIV-protease inhibitors and sialidase inhibitors, and in general to the development of antibacterial and antiviral drugs.
Planned learning activities and teaching methods:	All information will be available through the e-learning platform to the attending students. Besides lecturing, the course will use group works to stimulate soft skills scubas critical thinking, team work and peer evaluation.
Additional notes about suggested reading:	A reading list with detailed and thorough reviews will be provided for the students attending the course through the Moodle platform.
Textbooks (and optional supplementary readings)	Lemke, Thomas L.; Williams, David A.; Roche, Victoria F.; Zito, S. William, Foyeʼs principles of medicinal chemistryedited by Thomas L. Lemke, David A. Williamsassociate editors Victoria F. Roche, S. William Zito. Philadelphia [etc.]: Lippincott Williams & Wilkins, --. consultazione Wolff,-ME, Burger's Medicinal Chemistry and Drug Discovery. Hoboken: John Wiley & Sons, 1997. consultazione Nogrady, Thomas, Medicinal chemistrya biochemical approachThomas Nogrady. New York: Oxford University Press, 1988. consultazione Graham, Patrick, <<An >>introduction to medicinal chemistryGraham L. Patrick. Oxford: Oxford U.P., 2013. consultazione Silverman, Richard B., <<The >>organic chemistry of drug design and drug actionRichard B. Silverman. Amsterdam: Elsevier Academic Press, --. consultazione