- Docente: Anna Minarini
- Credits: 8
- SSD: CHIM/08
- Language: Italian
- Teaching Mode: Traditional lectures
- Campus: Bologna
- Corso: Single cycle degree programme (LMCU) in Chemistry and Pharmaceutical Technologies (cod. 8412)
Learning outcomes
The course deals with the fundamental strategies of design and synthesis of drugs and with the molecular mechanism of drug action. the chemical structures of drugs interacting with enzymes and receptors and their structure-activity relationship. Particularly the student will be learn the principal classes of agents acting on central and peripheral nervous systems.
Course contents
Neurotransmitter receptors
The bonding of ligands to receptors. Structure and classification of receptors. General mode of operation. Ligand-response relationships: agonist and antagonist concentration-response relationships, partial agonism, inverse agonism. Ligand-receptor theories: Clark's occupancy theory, the rate theory, two-state model, perturbation theory. Classification, localization, function, structure, active site of adrenergic receptors, cholinergic receptors, dopaminergic receptors, GABAergic receptors, and opioid receptors.
Neurotransmitters
Acetylcholine, catecholamines, serotonin, histamine, 4-aminobutyric acid, enkephalins: biosynthesis, release, uptake, metabolism, molecular properties, active conformation, stereochemical properties.
Drugs acting at neurotransmitter receptors
Structure-activity relationships, mechanism and site of action, therapeutic use, side effects, stereochemistry, and synthetic aspects of drugs acting at adrenergic, dopaminergic, cholinergic, serotoninergic, histaminergic, GABAergic, and opioid systems. Stereochemistry and synthesis of selected drugs.
Drug design
Basic principles of rational drug design. Drug design strategies. Modification of a lead compound.Readings/Bibliography
Chimica Farmaceutica, a cura di A.Gasco, F. Gualtieri, C. Melchiorre- Casa Editrice Ambrosiana, 2014
T. L. Lemke, D. A. Williams et al. - Foye's Principi di Chimica Farmaceutica - Piccin, Padova, 2014
C. Melchiorre - I recettori dei neurotrasmettitori: un'introduzione per la chimica farmaceutica - CLUEB, Bologna, 1996.
C. Melchiorre, A. Minarini, M. Recanatini, V. Tumiatti, M.L. Bolognesi - I recettori colinergici - CLUEB, Bologna, 1997.
F. Gualtieri, M.N. Romanelli, E. Teodori - Chimica farmaceutica dei recettori: disegno e sintesi di farmaci e mezzi di indagine farmacologica - CLUEB, Bologna, 1997.
M. Giannella, W. Quaglia - I recettori adrenergici - CLUEB, Bologna, 1998.
G. Ronsisvalle, M. Pappalardo, L. Pasquinucci, O. Prezzavento – I recettori oppioidi – CLUEB, Bologna, 1999.
D. Lednicer, L. A. Mitscher - The organic chemistry of drug synthesis, Voll. 1-6 - John Wiley & Sons, New York, 1977, 1980, 1984, 1990, 1995, 1999.
Assessment methods
As a preliminary test, the student should describe the synthesis of
two drugs among those in the program. If this test is passed, the
examination continues with a discussion on three topics of the
course drawn from the student. The registration on AlmaEsami is
required.
Office hours
See the website of Anna Minarini