Biophysical Chemistry

Recommended Prerequisites

BSc in Medicinal Chemistry, Chemistry, Biochemistry, Bioanalytical Sciences Medical Sciences.

Teaching Methods

Theoretical classes with the presentation of the syllabus indicated. Practical classes with resolution and discussion of several relevant problems.

Learning Outcomes

Understand the physico-chemical factors that establish the bioavailability and bioactivity of pharmaceuticals and small molecules with relevance in medicine.

Structure and dynamics of natural barriers that limit the absorption of the active molecules and their accumulation in the target tissues – cellular biomembranes, endothelia and epithelia.

Understand the processes of enzymatic catalysis.

Knowledge of QSAR techniques – quantitative relations between structure and activity – applied to small molecules with medical relevance.

Acquire operational skills regarding the stability of pharmacological agents.

Work Placement(s)

No

Syllabus

1. Biophysical characterization of cellular membranes with special emphasis to their properties as semi-permeable barriers.

2. Structure and physico-chemical properties of endothelia and epithelia, namely tight endothelia such as the blood-brain barrier.

3. Sequestration of small molecules by blood components – physico-chemical characterization of the binding agents and consequences in the bioavailability of drugs and biological ligands with medicinal relevance.

4. Quantitative relations between the structure of small molecules and their bioavailability and biological activity: a) acid-base properties b) solubility (aqueous media, non-polar solvents and biomembranes) c) binding to proteins

5. Enzymatic Catalysis. Catalysis mechanisms and enzyme inhibition.

6. Reaction kinetics in solution and in the solid state. Kinetics in micro-heterogeneous systems. Effect of temperature and humidity. Methods of shelf life determination.

Head Lecturer(s)

Maria João Pedrosa Ferreira Moreno Silvestre

Assessment Methods

Assessment
Resolution Problems: 25.0%
Exam: 75.0%

Bibliography

“Biological membranes: Theory of transport, potentials and electric impulses”, Ove Sten-Knudsen, Cambridge University Press. 2002, ISBN 9780521036351.

“Molecular Biophysics: Structures in Motion”, Michel Daune, Oxford University Press. 1999, ISBN:0198577826

“Drug bioavailability. Estimation of solubility, permeability, absorption, and bioavailability”, Han van de Waterbeemd, Hans Lennernäs, and Per Artursson, Wiley-VCH. 2003, ISBN:352730438X

“Drug Stability: Principles and Practices”, Jens T. Carstensen and Christopher Rhodes, Marcel Dekker, Inc. 2000, ISBN:0824703766