Learning outcomes of the course unit
AT the end of the course, the student should be able to:
Knowledge and understanding: To be acquainted with the chemical and the physico-chemical bases that regulate the operation of receptors; to understand the mechanisms through which small molecules activate or block nuclear or membrane receptors
Applying knowledge and understanding: The student must show to be able to synthesize their knowledge, their ability to analyze and understand the structure-activity relationships for classes of drugs through devising and sustaining critical arguments in the field of medicinal chemistry, proving to be able to have a professional approach to discipline
In addition, the teaching aims to achieve autonomy of judgment and Communicative Abilities.
Making judgments: Students will be able during the lessons, to interact with the themes suggested by the teacher and, even with the help of the recommended texts and teaching materials, be able to make independent judgments
Communication skills: The student must be able to clearly and critically present the results of their individual calculations, demonstrating knowledge of research topics carried out during the program
Learning skills: to be acquainted with a method of study and analysis that is tailored on the student and efficient, in order to extend the field of knowledge to different disciplines and in order to make his preparation suitable to higher-learning experiences.
Comprehension of the process leading to the synthesis of a molecule with biological action. Ability to make a retrosynthetic analysis and understand the most effective and rapid synthesis. Comprehension of the principal chemical reactions leading to the synthesis of therapeutic agents.
Organic Chemistry , Medicinal Chemistry , Biochemistry , Physiology , Pharmacology
Course contents summary
1) Structure of receptors
- Binding receptor/molecule of interest
- inhibition of receptors
- In-depth analysis of peculiar classes of receptors
2) Nuclear receptors
- molecular basis
- definition of a steroid hormone
- nomenclature and chemical structure of steroid hormones
- biosynthesis of steroid hormones
- mechanism of action of steroid hormones
- Biosynthesis of corticosteroids and mineralcorticoids
- Physiologic roles of corticosteroids
- Pathologies related to corticosteroids
- Relevant corticosteroids and Structure Activity Relationships
- Corticosteroids not steroid
- Synthetic procedures for the synthesis of the principal corticosteroids
- Mineralcorticoids. Physiopathological roles and therapeutic use.
4) Female sex hormones
- Biosynthesis of estrogens and progestins
- Physiologic roles of progestins
- Progestinic agents
- Relevant progestins and Structure Activity Relationships
- Progestins antagonists
- Birth pill
- Marker degradation
- Synthesis of noretindrone
- Estrogens, physiological roles
- Non-steroid estrogens
-Antiestrogens: therapeutic role
- Inhibitors of aromatase.
5) Male sex hormones
- Biosynthesis of testosterone
- Physiological roles of testosterone
- Anabolic androgens
- Reverse anorexia
- Relevant androgens and Structure Activity Relationships
- Main androgens
- Non steroid androgens
6) Hyperlipoproteinemia and cardiovascular disease
- the cholesterol and other blood lipids
- cholesterol biosynthesis
- metabolic syndrome
- Drugs against obesity and hyperlipidemic
HMG - CoA reductase inhibitors ( statins )
- diabetes and insulin
- Antidiabetic drugs
7) Bile acids
- Biosynthesis of bile acids
- Physio pathologic roles of bile acids
- Structure of bile acids and interaction with FXR
- Obeticholic acid
- other FXR agonists
The Following synthetic procedures will be showed and commented.
- Marker degradation
- Obethicholic acid
- Cortisone e corticosteroids
Gragam L. Patrick ,
III edition Edises
According to the COVID emergence, the course will be conducted through blended learning. Lectures will be made in the teaching room, provided reservation , and at the same time in streaming with TEAMS platform. Interactions with students will be made possible through questions by the teacher.
Each lesson is a teaching module unit , in which , for each topic , are given to the student the foundation for acquiring knowledge and understanding , and to apply the knowledge and understanding to the problem treated in the unit of learning module
Teaching material will be made available on Elly. It will be made of slides and scientific article variously selected.
Assessment methods and criteria
The final evaluation will be based on a oral exam in teleconference. This until the COVID emergence will be declared finished by the responsible bodies and social distancing abolished.
The final exam will be made open questions, and in same cases, students will be asked to draw and/or describe the mechanism of some reactions, or the synthesis of molecules of interest.
To each answer will be applied a score, that can be also negative if the answer is not correct.
The exam is passed when the final score is equal or more than 18/30