Learning objectives
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.
Prerequisites
Organic Chemistry , Medicinal Chemistry , Biochemistry , Physiology , Pharmacology
Course unit content
1) Structure of Receptors
• Receptor/molecule of interest binding
• Receptor inhibition
• In-depth analysis of particular receptor classes common in Pharmaceutical Chemistry
• Nuclear Receptors
• Classification
• Structure
• Molecular bases of transcriptional activity
o Definition of a steroid hormone
o Nomenclature and chemical structure of steroid hormones
o Biosynthesis of steroid hormones
o Mechanism of action of steroid hormones
2 Introduction to Hormones
• Introduction to Cholesterol
• Biosynthesis of Cholesterol
• Lipoproteins
• Hyperlipoproteinemia and cardiovascular diseases
• Drugs active against hypercholesterolemia
• HMG-CoA reductase inhibitors (Statins)
o Structure
o RAS statins
3 Diabetes and Metabolic Disease
• Drugs for the treatment of diabetes
o Type 1 diabetes
o Type 2 diabetes
• Oral hypoglycemics
o Structure and mechanism of action
4 Female Sex Hormones
• Biosynthesis
• Mechanism of action
• Progesterone
o Marker degradation
o Progesterone synthesis
o The contraceptive pill
• Estrogens
o History and use
o Non-steroidal agonists
• SERMs
o Aromatase and mechanism of action
o Reversible and irreversible aromatase inhibitors
5 Male Sex Hormones
• Biosynthesis
• Mechanism of action
• Anabolics
• Doping
• RAS androgens
• Reverse anorexia
6 Corticosteroids
• Biosynthesis
• Metabolism
• Metabolic syndrome
• Pharmacokinetics
• RAS corticosteroids
7 Bile Acids
• Biosynthesis
• Structure and RAS
• Therapeutic activity
8 List of selected Syntheses:
• EZETIMIBE
• FLUVASTATIN
• ROSIGLITAZONE
• PROGESTERONE (MARKER DEGRADATION)
• NORETHINDRONE
• DIETHYLSTILBESTROL
• TAMOXIFEN
• TESTOSTERONE
• FINASTERIDE
• STRATEGIES FOR CORTISONE SYNTHESIS
• OBETICHOLIC ACID
Full programme
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Bibliography
Gragam L. Patrick ,
Pharmaceutical Chemicals,
III edition Edises
Teaching methods
The course will be conducted through lectures. 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
Assessment methods and criteria
The summative assessment of learning is conducted through a final ORAL exam. The student will be required to answer questions related to the subjects covered. In some cases, the questions will involve drawing or writing structures of interest or reaction mechanisms. Additionally, the candidate will be required to answer at least one question on the synthesis of the selected molecules. The exam is considered passed if the grade is equal to or greater than 18/30.
Other information
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