GENERAL PHARMACEUTICAL CHEMISTRY AND LABORATORY
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- Versione italiana
- Academic year
- 2017/2018
- Teacher
- RICCARDO RONDANIN
- Credits
- 6
- Didactic period
- Primo Semestre
- SSD
- CHIM/08
Training objectives
- The course will allow the students to understand how different functional groups lead to the peculiar pharmacokinetic and pharmacodynamic properties of a drug: lipophilic/hydrophilic rate, ionization, solubility, chemical and metabolic stability, interaction with enzymes and receptors. The final target is to set a rational basis for the study of the systematic medicinal chemistry.
The laboratory part of the course is focused to furnish the theoretical and methodological fundamentals, as well as the technical/practical skills for the preparation and volumetric standardization of some common reagent’s solutions, together with an example of instrumental analytical methodology. Moreover, students will be engaged in some basic operations of organic chemistry, including purification and quality control of a reaction product. At the end, the student should be able to know and correctly use the basic tools present in a chemical analysis and research laboratory. Prerequisites
- Knowledge of the topics of courses on Mathematics, Physics, General and Organic Chemistry
Course programme
- Laboratory part
General introduction to the analytical process and general methodologies in organic chemistry. Stoichiometric calculations, mass and volume measurements. Acid-base, and redox equilibria titrations. Titrations curves. Accuracy and precision. Fundamental operations and general equipment in a chemical laboratory. Use of analytical balance. Preparation of solutions of common reagents and standardization with volumetric methodologies. Evaluation of results.
Electrical conductivity of solutions and laws of conductivity. Conductivity cells and conductimeter. Direct and indirect conductimetry. Instrumentation. Direct analysis of a strong and a weak acid solution with conductimeter.
Basic operations in organic chemistry laboratory. Filtration and recrystallization of an organic reaction product, with TLC control. Theorical basis of chromatographic separations, and TLC laboratory practice with samples of different compounds mixtures.
General Medicinal Chemistry part.
Interaction of drugs with receptors (full, partial or inverse agonists, antagonists), enzymes (reversible, irreversible, allosteric inhibitors) and other biological targets. Selectivity toward different isozymes and receptor subtypes. How drugs bind with their target, polar and non-polar binding interactions.
Physicochemical properties of drugs and relation between biological ADME behavior and structural features.
Drug distribution, acid-base properties. Lipophilicity definitions and lipophilicity scales. Ionization rate, water solubility, definition and calculation of logP and logD. Main metabolic phases 1 and 2 transformations. Prodrugs and bioprecursors strategy.
The drug discovery process. Strategy and tactics in drug discovery. Target identification and validation, lead identification. Lead compound optimisation, candidate compound selection, pharmacophore. Isostery and bioisostery. Didactic methods
- Lectures for in total 32 hours: 16 dedicated to laboratory exercitations theory and 16 dedicated to the general medicinal chemistry program.
Laboratory class for in total 24 hours, divided into 6 sessions. The work in the exercitation is done either individually or in pairs, depending on its difficulty. Learning assessment procedures
- Written examination and laboratory reports.
Written examination is consisting of 1) discussions about theoretical topics about both laboratory and general medicinal chemistry parts; 2) finding the solution of problems regarding properties of a drug, by evaluating its structure and functional groups and/or data treatment from a simulated laboratory analysis.
If the written examination results positive, the final mark will be modified, but not averaged, by taking into consideration also the evaluation of the laboratory reports. Reference texts
- Lecture’s notes.
Patrick G. L. Chimica Farmaceutica. III Edizione. EdiSES.
Williams D.A.; Lemke T.L. Foye’s Principi di Chimica Farmaceutica. VI Edizione, Piccin.
Greco G. Farmacocinetica e Farmacodinamica su Basi Chimico-Fisiche. Loghìa.
Silverman R. B., Holladay M. W. Manuale di chimica farmaceutica. Edra.
Stevens E. Chimica Farmaceutica. I processi di scoperta dei farmaci. Piccin.
Block, J.H., Beale, J.M. Wilson and Gisvold’s Textbook of Organic and Pharmaceutical Chemistry. XI Edition, Lippincott Williams & Wilkins Edition.
Savelli F., Bruno O. Analisi Chimico Farmaceutica. Piccin.
