SYNTHESIS AND PROPERTIES OF BIOLOGICALLY ACTIVE COMPOUNDS PART B

Degree course: 
Corso di Second cycle degree in CHEMISTRY
Academic year when starting the degree: 
2018/2019
Year: 
2
Academic year in which the course will be held: 
2019/2020
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, biochemistry and heterocyclic chemistry is a pivotal prerequisite.

The final evaluation consists of an oral interview in which the students will be examined on all the topics tackled in the lectures.
The final mark is the average of the two partial evaluations.

Assessment: 
Voto Finale

The course aims at furnishing:
- knowledge of selected topics in the field of the medicinal chemistry;
- knowledge of the most important synthetic methodologies of selected drugs and their characterization;
- details of industrial methodologies for the synthesis of some drugs.

Antibacterial agents (12 hours). The bacterial cel and mechanisms of antibacterial action. Antimetabolites: sulphonamides. Antibacterial agents which inhibit cell wall synthesis: penicillins, cephalosporins, other -lactam antibiotics(clavulanic acid, carbapenem e monobactams), and glycopeptides. Antibacterial agents which impair protein synthesis: aminoglycosides, tetracyclines, chloramphenicol, macrolides, oxazolidinones. Agents which act on nucleic acid transcription and replication.

Antiviral agents (8 hours). Antiviral drugs used against DNA viruses. Antiviral drugs acting against RNA viruses: HIV, flu virus, cold virus, hepatitis C.

Drugs acting on the adrenergic nervous system (PNS) (6 hours). Catecholamines: biosynthesis, metabolism and structure activity relationship. Adrenergic agonists: 2-agonists and the treatment of asthma. Adrenergic receptor antagonists: -blockers as cardiovascular drugs. Structure activity relationship of aryloxypropanolamines. Benzodiazepines.

The opioid analgesics (6 hours). Morphine: structure-activity relationship. Morphine analogues: drug extension, simplification or drug dissection, rigidification. Morphine antagonists.

Antibacterial agents (12 hours). The bacterial cel and mechanisms of antibacterial action. Antimetabolites: sulphonamides. Antibacterial agents which inhibit cell wall synthesis: penicillins, cephalosporins, other -lactam antibiotics(clavulanic acid, carbapenem e monobactams), and glycopeptides. Antibacterial agents which impair protein synthesis: aminoglycosides, tetracyclines, chloramphenicol, macrolides, oxazolidinones. Agents which act on nucleic acid transcription and replication.

Antiviral agents (8 hours). Antiviral drugs used against DNA viruses. Antiviral drugs acting against RNA viruses: HIV, flu virus, cold virus, hepatitis C.

Drugs acting on the adrenergic nervous system (PNS) (6 hours). Catecholamines: biosynthesis, metabolism and structure activity relationship. Adrenergic agonists: 2-agonists and the treatment of asthma. Adrenergic receptor antagonists: -blockers as cardiovascular drugs. Structure activity relationship of aryloxypropanolamines. Benzodiazepines.

The opioid analgesics (6 hours). Morphine: structure-activity relationship. Morphine analogues: drug extension, simplification or drug dissection, rigidification. Morphine antagonists.

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 any day by previous appointment.