SYNTHESIS AND PROPERTIES OF BIOLOGICALLY ACTIVE COMPOUNDS PART B
- Overview
- Assessment methods
- Learning objectives
- Contents
- Full programme
- Teaching methods
- Contacts/Info
A deep knowledge of the fundamentals of organic chemistry, biochemistry and heterocyclic chemistry is a pivotal prerequisite.
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. The final mark is the average of the two partial marks.
The course is structured in two parts 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 (6 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 (4 hours). Morphine: structure-activity relationship. Morphine analogues: drug extension, simplification or drug dissection, rigidification. Morphine antagonists.
Anti-ulcer agents (4 hours). Factors influencing the release of gastric acid: Cimetidine and ranitidine. Proton pump inhibitors: Omeprazole.
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 (6 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 (4 hours). Morphine: structure-activity relationship. Morphine analogues: drug extension, simplification or drug dissection, rigidification. Morphine antagonists.
Anti-ulcer agents (4 hours). Factors influencing the release of gastric acid: Cimetidine and ranitidine. Proton pump inhibitors: Omeprazole.
The teaching activities consist of classroom lecturing using PPT support
Professors are available to meet the students any day by previous appointment.