SYNTHESIS AND PROPERTIES OF BIOLOGICALLY ACTIVE COMPOUNDS PART A

Degree course: 
Corso di Second cycle degree in CHEMISTRY
Academic year when starting the degree: 
2020/2021
Year: 
2
Academic year in which the course will be held: 
2021/2022
Course type: 
Supplementary compulsory subjects
Credits: 
4
Period: 
First Semester
Standard lectures hours: 
32
Detail of lecture’s hours: 
Lesson (32 hours)
Requirements: 

A deep knowledge of the fundamentals of organic chemistry, biochemsitry and heterocyclic chemistry is a pivotal prerequisite.

The final examination consists of two oral interviews, in which the students will be examined on all the topics tackled in the each module lectures.
The final mark is the average of the two partial evaluations.

Assessment: 
Voto Finale

The course is composed of two modules. In Part A, students will be made familiar with the principles of pharmacodynamics, pharmacokinetics and the process of drug discovery .

Drug targets: proteins, enzymes and receptors (12 h). Intermolecular binding forces: Protein structure: primary, secondary (alpha-helics, beta turns and beta-sheets) and tertiary. Enzymatic interactions and catalytic role of enzymes. Receptors: neurotransmitters and hormones, receptor activation and signal transduction.
Pharmacodynamics and pharmacokinetics (12 h): reversible, irreversible and allosteric inhibitors. Agonists, antagonists and partial agonists, affinity efficacy and potency. Pharmacokinetics: drug absorption, distribution, metabolism and excretion.
Drug discovery and development (8 h): choosing a drug target, identifying a bioassay, finding a lead compound. Structure optimization e drug formulation. Preclinical and clinical phases.

Drug targets: proteins, enzymes and receptors (12 h). Intermolecular binding forces: Protein structure: primary, secondary (alpha-helics, beta turns and beta-sheets) and tertiary. Enzymatic interactions and catalytic role of enzymes. Receptors: neurotransmitters and hormones, receptor activation and signal transduction.
Pharmacodynamics and pharmacokinetics (12 h): reversible, irreversible and allosteric inhibitors. Agonists, antagonists and partial agonists, affinity efficacy and potency. Pharmacokinetics: drug absorption, distribution, metabolism and excretion.
Drug discovery and development (8 h): choosing a drug target, identifying a bioassay, finding a lead compound. Structure optimization e drug formulation. Preclinical and clinical phases.

An Introduction to Medicinal Chemistry, G. L. Patrick, Oxford, 5th Ed.

The teaching activities consist of classroom lecturing

Professors are available to meet the students upon by previous appointment by e-mail.