First cycle
degree courses
Second cycle
degree courses
Single cycle
degree courses
School of Medicine
Course unit
MEP5070482, A.A. 2017/18

Information concerning the students who enrolled in A.Y. 2017/18

Information on the course unit
Degree course Second cycle degree in
ME2193, Degree course structure A.Y. 2015/16, A.Y. 2017/18
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Number of ECTS credits allocated 7.0
Type of assessment Mark
Course unit English denomination DRUG DISCOVERY AND DEVELOPMENT
Department of reference Department of Pharmaceutical and Pharmacological Sciences
E-Learning website
Mandatory attendance
Language of instruction English
Single Course unit The Course unit can be attended under the option Single Course unit attendance
Optional Course unit The Course unit can be chosen as Optional Course unit

Teacher in charge BARBARA GATTO CHIM/08

ECTS: details
Type Scientific-Disciplinary Sector Credits allocated
Core courses CHIM/08 Pharmaceutical Chemistry 7.0

Course unit organization
Period Second semester
Year 1st Year
Teaching method frontal

Type of hours Credits Teaching
Hours of
Individual study
Lecture 7.0 56 119.0 No turn

Start of activities 26/02/2018
End of activities 01/06/2018
Show course schedule 2019/20 Reg.2015 course timetable

Examination board
Board From To Members of the board
5 Commissione a.a. 2019/20 02/12/2019 30/09/2020 GATTO BARBARA (Presidente)
MORO STEFANO (Membro Effettivo)
4 Commissione a.a. 2018/19 03/12/2018 30/09/2019 GATTO BARBARA (Presidente)
MORO STEFANO (Membro Effettivo)
3 Commissione a.a. 2017/18 01/12/2017 30/09/2018 GATTO BARBARA (Presidente)
MORO STEFANO (Membro Effettivo)

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. 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: Usually exam is an oral discussion; modality might change upon discussion/decision with the class during the course
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
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, Foye╩╝s principles of medicinal chemistryedited by Thomas L. Lemke, David A. Williamsassociate editors Victoria F. Roche, S. William Zito. Philadelphia [etc.]: Lippincott Williams & Wilkins, --. consultazione Cerca nel catalogo
  • Wolff,-ME, Burger's Medicinal Chemistry and Drug Discovery. Hoboken: John Wiley & Sons, 1997. consultazione Cerca nel catalogo
  • Nogrady, Thomas, Medicinal chemistrya biochemical approachThomas Nogrady. New York: Oxford University Press, 1988. consultazione Cerca nel catalogo
  • Graham, Patrick, <<An >>introduction to medicinal chemistryGraham L. Patrick. Oxford: Oxford U.P., 2013. consultazione Cerca nel catalogo
  • Silverman, Richard B., <<The >>organic chemistry of drug design and drug actionRichard B. Silverman. Amsterdam: Elsevier Academic Press, --. consultazione Cerca nel catalogo