Medicinal Chemistry
1° Year of course - Second semester
Frequency Not mandatory
- 6 CFU
- 48 hours
- Italian
- Trieste
- Opzionale
- Oral Exam
- SSD CHIM/08
1. Knowledge and understanding: the student will acquire knowledge of medicinal chemistry, concerning the design and development of drugs, with particular attention to structure-activity relationships, combinatorial approaches to the identification of new compounds and knowledge related to different classes of drugs such as antibacterial, antiviral, antitumor, and antialzheimer compounds. 2. Ability to apply knowledge and understanding: the student will be able to apply the knowledge acquired in point 1 in the analysis of the chemical structures and the activity of the compounds belonging to the aforementioned classes of drugs. 3. Judgment autonomy: the student will be able to autonomously understand the principles that lead to the development of a molecular structure and to correlate the knowledge of the general approaches of the drug development to specific classes of drugs as the ones previously mentioned. 4. Communication skills: the student will be able to clearly explain the concepts acquired in point 1 demonstrating conceptual accuracy, linguistic accuracy and judgment autonomy. 5. Learning skills: the student will be able to autonomously study the topics covered in the course, also consulting specific bibliography.
Good knowledge of organic chemistry
This course is focused on the medicinal chemistry's basic concepts. Special interest will be devoted to the study and comprehension of the most important macromolecular targets for drugs, the drug/target interactions, the relationships between chemical structure and pharmacological activity and the molecular mechanisms involved in the drug activity. Examples of development of: Antibacterial, antiviral, antialzheimer, and antitumoral drugs. The content of the teaching corresponds to the educational objectives stated in Article 4 and Annex C of the Teaching Regulations of the Course of Studies.
Chimica Farmaceutica a cura di A. Gasco, F. Guarltieri, C. Melchiorre Casa Editrice Ambrosiana Graham L. Patrick An introduction to Medicinal Chemistry 4th edition Oxford University Press Greco Farmacocinetica e Farmacodinamica su Basi Chimico-Fisiche Loghia Victoria F. Roche S. William Zito Thomas L. Lemke David A. Williams Foye's Principle of Medicinal Chemistry 8th Edition Wolters Kluwer
Introduction and definitions of medicinal chemistry, drug etc. From lead compound to drug: approaches toward the discovery of clinically useful molecules Physical-chemical parameters, which influence drug access to the target of action. Biological targets: enzymes, structural and carrier proteins, nucleic acids. Receptors and drugs. Agonism and antagonism. Receptor theories. Stereochemistry of drugs and biological connotations. Isostery and bioisostery. Drug metabolism aspects. Combinatorial chemistry and dynamic combinatorial chemistry. Innovative approaches in drug design. Examples of drug development. Antibacterial drugs Antiviral drugs Anti-Alzheimer approaches Antitumor drugs.
Lectures with the support of power point presentations, black board, short movies, Wooclap, Kahoot. Material is available at the moodle site of the course. Any changes to the methods described here that may be necessary to ensure the application of safety protocols in the context of possible emergency situations will be announced on the Department website, the Course of Study and on the Moodle page for teaching.
For further information, please directly contact the professor in charge of this course. email: daros@units.it phone: 040558 3597 Any changes to the methods described here, which will be necessary to ensure the application of safety protocols related to any emergency situations, will be communicated on the Department website, the Degree Course website and on the Moodle page of the course.
Written examination. More specifically, the written test will be based on 7-9 open questions about the general knowledge of Medicinal Chemistry and the various drugs' families presented during the course. The result of the exam will be evaluated with a score of thirty points based on the following criteria: -Excellent (30-30 cum laude): excellent knowledge of the topics, excellent language skills, excellent analytical skills; the student is able to brilliantly apply theoretical knowledge to concrete cases. -Very good (27-29): good knowledge of the topics, remarkable language skills, good analytical skills; the student is able to correctly apply theoretical knowledge to concrete cases. -Good (24-26): good knowledge of the main topics, good language skills; the student shows adequate ability to apply theoretical knowledge to concrete cases. - Satisfactory (21-23): The student does not fully master the main topics of teaching, but has the basic knowledge; however, he/she demonstrates satisfactory language skills and an adequate ability to apply theoretical knowledge to concrete cases. -Sufficient (18-20): minimal knowledge of the main topics of teaching and technical language, limited ability to adequately apply theoretical knowledge to concrete cases. - Insufficient (<18): The student does not have acceptable knowledge of the content of the various topics of the teaching course. Any changes to the methods described here that may be necessary to ensure the application of safety protocols in the context of possible emergency situations will be announced on the Department website, the Course of Study and on the Moodle page for teaching.
This course explores topics closely related to one or more goals of the United Nations 2030 Agenda for Sustainable Development (SDGs)