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Course unit
DRUG DISCOVERY AND DEVELOPMENT
MEP5070482, A.A. 2017/18
Information concerning the students who enrolled in A.Y. 2017/18
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 |
Hours of Individual study |
Shifts |
Lecture |
7.0 |
56 |
119.0 |
No turn |
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)
SISSI
CLAUDIA
(Supplente)
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4 Commissione a.a. 2018/19 |
03/12/2018 |
30/09/2019 |
GATTO
BARBARA
(Presidente)
MORO
STEFANO
(Membro Effettivo)
SISSI
CLAUDIA
(Supplente)
|
3 Commissione a.a. 2017/18 |
01/12/2017 |
30/09/2018 |
GATTO
BARBARA
(Presidente)
MORO
STEFANO
(Membro Effettivo)
SISSI
CLAUDIA
(Supplente)
|
Prerequisites:
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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:
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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:
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Usually exam is an oral discussion; modality might change upon discussion/decision with the class during the course |
Assessment criteria:
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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:
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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:
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All information will be available through the e-learning platform to the attending students |
Additional notes about suggested reading:
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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) |
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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
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Wolff,-ME, Burger's Medicinal Chemistry and Drug Discovery. Hoboken: John Wiley & Sons, 1997. consultazione
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Nogrady, Thomas, Medicinal chemistrya biochemical approachThomas Nogrady. New York: Oxford University Press, 1988. consultazione
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Graham, Patrick, <<An >>introduction to medicinal chemistryGraham L. Patrick. Oxford: Oxford U.P., 2013. consultazione
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Silverman, Richard B., <<The >>organic chemistry of drug design and drug actionRichard B. Silverman. Amsterdam: Elsevier Academic Press, --. consultazione
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