Learning objectives
The course provides basic notions on the principles of medicinal chemistry, on the chemical, physico-chemical and structural properties influencing drug action, and on the mechanism of action of the most important classes of drugs. Examples of biotechnology drugs or of drugs whose design and development were based on the application of biotechnological techniques will be treated.
Prerequisites
Basic notions of organic chemistry and biochemistry
Course unit content
<p><u><strong>Principles of medicinal chemistry</strong></u> <br />
Naming of drugs <br />
Classification of drugs <br />
Moments of drug action: pharmaceutical, pharmacokinetic and pharmacodynamic phases. <br />
Chemical and physico-chemical properties influencing drug action: chemical reactivity, lipophilicity, ionization, solubility. <br />
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<strong>Pharmacodynamics</strong> <br />
Drug targets and their mechanism of action: <br />
· enzymes; <br />
· receptors; <br />
· nucleic acids, <br />
· lipids. <br />
<br />
<strong>Pharmacokinetics</strong> <br />
Drug absorption and distribution, binding to proteins. <br />
Drug metabolism: phase I and phase II transformations. <br />
Drug excretion <br />
Prodrugs <br />
<br />
<br />
<u><strong>Selected examples of drugs</strong></u> <br />
Monoclonal antibodies and immunoconjugates. <br />
Antisense oligonucleotides <br />
Proteins: insulin <br />
Ribozymes <br />
Soluble receptors <br />
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</p>
Full programme
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Bibliography
G. L. Patrick: "An Introduction to Medicinal Chemistry"; Third Edition, Oxford University Press, Oxford, 2005. ISBN: 0-19-927500-9 <br />
<br />
D. A. Williams, T. L. Lemke: “Foye’s Principi di Chimica Farmaceutica” PICCIN, Padova, 2005. ISBN: 88-299-1726-5 <br />
<br />
C. G. Wermuth: "The practice of Medicinal Chemistry" Second Edition, Elsevier Academic Press, Amsterdam, 2003. ISBN: 0-12-744481-5 <br />
Teaching methods
The oral exam at the end of the course will cover all the topics treated during the lessons. The student has to demonstrate that he/she has understood and is able to discuss the importance of the major concepts of each topic.
Assessment methods and criteria
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Other information
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