Pharmaceutical Biotechnology

Drug design basis: hit and lead compounds. Target validation. Pharmacodynamic and pharmacokinetics. HTS approach. Combinatorial chemistry in drug design. Structure activity relationships and physico-chemical basis of drug activity. Classical methods in drug design: vinilogy, isostery and scaffold hopping. Modern methods in drug design: Pharmacophoric approac, QSAR and 3-D QSAR, Molecular Docking, COMBINE. Chemometry and Proteochemometry. Drug design through virtual screening

The students should have acquired the content of all courses followed in the previous years with particular indication to all chemisty based and biochemistry courses. Medicinal chemistry rely on fundamental courses and therefore it is very important their knowledge

- Foye. Principles of medicinal chemistry. - Patrick. An Introduction to Medicinal Chemistry. - Burger. Drug Discovery. - Wermuth. The Practice of Medicinal Chemistry. - Comprehensive Medicinal Chemistry II. - PDF of the lectures available on the elearning platform (https://elearning.uniroma1.it/course/view.php?id=441)

Attendance is in face to face

The student will make a written part that will not exclude him/her to the oral exam, but will be used for the final evaluation. To access to the final exam the studen have to prepare a MS Word or LibreOffice document and MS powerpoint o LibreOffice Impress presentation containing only the content of the Word document. The document, the presentation and all the material used and produced to access the exam must be shared with the teacher in a the Google Drive folder The student will be asked to apply the medicinal chemistry techniques in drug design to a series of small molecules of known activity and structures against a target structure of his/her choice. During the exam the student will discuss, through a power point (microsoft) / impress (libreoffice) presentation the results of his application. The student should also show the numerical results and should prove to have acquired the practical and theoretical aspects to design new bioactive molecules. Furthermore, to assess the theorical preparation the student have to make a writte part answering to a series of questions. The final mark will be a balance between the partecipation during the lectures, the written part and the final presentation.