CdSCHIMICA E TECNOLOGIA FARMACEUTICHE
|ADVANCED MEDICINAL CHEMISTRY||CHIM/08||LEZIONI||21|
The student will acquire knowledge about the chemical mechanism of action/activation of therapeutic agents.
Knowledge acquisition will be verified by written tests or oral examinations, where the student will be asked to solve specific problems or to illustrate a concept.
At the end of the course the student will be able to identify the principal mechanism of action/activation of several classes of therapeutic agents and of their prodrugs. Furthermore, he/she will be able to propose structural modification for the design of potentially more active/selective pharmaceuticals.
The abilities acquired by student to associate chemical structure and biopharmaceutical activity will be verified by means of specific questions present in either the written or the oral examination.
The student will learn to associate chemical structures with biopharmaceutical activities, as well as the possible chemical/biological mechanism for the selective activations of prodrugs, to be applied in the design of new perspective therapeutic agents.
The skills of the student to propose solutions to the interpretation of the data and to the design of innovative therapeutic agents will be verified during the examinations.
There are no compulsory propedeutics. However, the student will have to possess a deep knowledge of Medicinal Chemistry, Organic Chemistry and Biochemistry, in order to understand the topics if this course. Furthermore, a good command of the English language is required, since lectures are given in English.
The modality of this course is a Lecture-style instruction with the help of projected slides and drawings on the blackboard.
Molecular complexity, pharmacophoric elements, synthetic accessibility.
Correlations between chemical characteristics and biopharmacological properties.
Fragment-based drug design, ligand efficiency.
Prodrugs: structural design, removable/modifiable groups, enzymatic and non-enzymatic activation processes.
“Smart” prodrugs, hypoxia-selective bioreductively-activated prodrugs, enzyme- (ADEPT, MDEPT, PDEPT, etc.) and antibody- (ADAPT) mediated selective activations of prodrugs.
Polymer therapeutics. Soft-drugs (or Ante-drugs).
R. B. SILVERMAN: Organic Chemistry of Drug Design and Drug Action - 2nd Edition, Elsevier - Academic Press, San Diego, CA - USA, 2004. [ISBN 0-12-643732-7]
C. G. WERMUTH: The Practice of Medicinal Chemistry - 2nd Edition, Elsevier – Academic Press, London, UK, 2003. [ISBN 0-12-744481-5]
E. H. Kerns, L. Di: Drug-like Properties: Concepts, Structure Design and Methods – Academic Press / Elsevier, Burlington MA, USA, 2008. [ISBN 978-0-1236-9520-8]
Recent scientific articles that will be cited in class.
The exam consists in two written tests, which will be due after the first half of the classes and at the end of the classes, respectively.
Each written tests generally have three questions or problems to be solved.
The written tests will take place in normal classrooms and generally last two hours each.
The student passes the exam if he/she gets a minimum of 18/30 in each of these tests. The final marks are obtained as an average of the two tests.
Those students who are not willing/able to pass the written tests, will sustain an oral examination of about 45 minutes, where he/she will be asked to describe the subjects treated in the classes.