SYNTHESIS OF BIOLOGICALLY ACTIVE COMPOUNDS

Degree course: 
Corso di Second cycle degree in CHEMISTRY
Academic year when starting the degree: 
2017/2018
Year: 
2
Academic year in which the course will be held: 
2018/2019
Language: 
English
Credits: 
8
Period: 
First Semester
Standard lectures hours: 
64
Requirements: 

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

Final Examination: 
Orale

The final examination consist of two oral interviews, in which the students will be examined on all the topics tackled in the each module lectures.

Assessment: 
Voto Finale

The course is composed by two modules and aims at furnishing:
- knowledge of selected topics in the field of the medicinal chemistry;
- knowledge of the most important synthetic methodologies of selected organic compounds and their characterization;
- details of industrial methodologies for the synthesis of some compounds.

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.
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.