Teaching Methodologies
Theoretical Matrix:
Essentially expository methodology using the appropriate audiovisual means appealing to the student’s involvement.
Theoretical Practical Matrix:
Exercise resolution
Access to internet sites to search for articles and use some free available chemical structure design and molecular modeling programs. Laboratory work.
Continuous evaluation:
Theoretical Matrix e Theoretical Practical Matrix: 2 written tests (80% T+ 20% TP) (90% of the final evaluation)
The presence and participation of students in classes is valued (10% of the final evaluation)
Regular period Exam, Appeal period Exam and Special period Exam, in accordance with the Academic Regulation in force.
Learning Results
Objective 1 – Students must acquire knowledge of the study of drugs from a chemical point of view.
Objective 2 – Students should acquire knowledge about the basic principles used in drug design and development
Program
T:
1.Introduction to Pharmacochemistry:
Drugs and drugs targets
Intermolecular binding forces
Classification and nomenclature of drugs.
Drug targets (strucure and funcion): Proteins, Enzymes, Receptors, Nucleic acids, Lipids and Carbohydrates
2.Drug discovery: design and development
Drug discovery: finding a lead
SOSA approach
Drug design: Optimizing target interactions
Structure-activity relationships (SAR)
Isosteres
Identification of a pharmacophore
Drug design: Optimizing access to the target
Prodrugs to improve drugs
3.Computers in medicinal chemistry
Quantitative structure-activity relationships (QSAR): Physicochemical properties, Hansch equation.
QSAR 3D
TP:
Notions of drug chirality and its importance (Bases of isomerism)
Octanol/water partition coefficient
Laboratory work: “The influence of pH on drug absorption” and “Experimental Determination of logP”
Contact with design software for chemical structures and calculation of some properties
Internship(s)
NAO
Bibliography
Graham L. Patrick, An Introduction to Medicinal Chemistry, 5th Edition, Oxford University Press 2013.
Eliezer J. Barreiro e Carlos Alberto Manssour Fraga, Química Medicinal: As Bases Moleculares da Ação dos Fármacos, Artmed, 2008
SILVERMAN, R. B. – The organic chemistry of drug design and drug action. 2nd ed. Academic Press, 2004