Unit ADVANCED PHARMACEUTICAL CHEMISTRY

Course
Pharmaceutical biotechnologies
Study-unit Code
55178806
Location
PERUGIA
Curriculum
In all curricula
Teacher
Antonio Macchiarulo
Teachers
  • Antonio Macchiarulo
Hours
  • 42 ore - Antonio Macchiarulo
CFU
6
Course Regulation
Coorte 2022
Offered
2022/23
Learning activities
Affine/integrativa
Area
Attività formative affini o integrative
Academic discipline
CHIM/08
Type of study-unit
Obbligatorio (Required)
Type of learning activities
Attività formativa monodisciplinare
Language of instruction
Italian
Contents
The course will offer insights on specific topics that play a key role in the drug discovery process such as: discovery of an innovative biological target; the phases of designing and developing a new drug; preclinical experimentation. Particular attention will be given to the biotechnological approaches that affect the process of drug discovery and development. Several case studies will be addressed in the final part of the course to highlight how the topics covered in the course come to be integrated.
Reference texts
1) Patrick, Introduction to Medicinal Chemistry, IV edition.
2) Drugs: From Discovery to Approval, 2nd Edition Rick Ng (Editore: Wiley-Blackwell).
Educational objectives
The aim of the first part of the course is to provide major information on the approaches to target identification and validation in drug discovery. The aim of the second part of the course is to provide advanced knowledge on the methodologies and approaches to design and optimize chemical compounds on the route to drug candidates.
Prerequisites
The contents and objectives of the course will be fully acquired and achieved by students if they possess the following knowledge.
Essential knowledge that a student must possess at the beginning of the course:
- Bioorganix Chemistry; Pharmacology; Biology.
Skills which the student must have at the beginning of the course:
- Molecular Biology; Bioinformatics
Useful knowledge that a student must possess at the beginning of the course:
- Mathematics (statistics); English.
Teaching methods
Frontal and/or remote lectures on all topics of the course.
Other information
The main knowledge gained will be:
- Methods to identify and validate a biological target.
- Design and synthesis of chemical libraries according to the concepts of molecular diversity and drug-likeness.
- Approaches to discover a "Lead compound" and optimize its pharmacodynamic and pharmacokinetic properties.
- Methods to study ligand / target interaction.
The main skills that will be acquired at the end of the course include:
- Ability to set up an experimental study aimed to discover new biological targets.
- Analyze the process of drug discovery identify problems and perform risk assessment.
- Design a chemical library of drug-like compounds.
- Appropriate communication skills in correct scientific terminology.
Learning verification modality
The exam includes an oral exam consisting of a discussion lasting about 30 minutes aimed at ascertaining the extent of the level of understanding reached by the student and his depth of understanding in the topics of the program.
In addition, it will be evaluated the ability to speak with propriety of language and organization of the subject exposed.

See also http://www.unipg.it/disabilita-e-dsa
Extended program
Pre-genomic and post-genomic approaches to target validation. Receptors as drug targets. Enzyme as drug target. Protein-protein interactions as drug target. High thorough-put screening. Combinatorial chemistry and parallel chemistry. Molecular modelling. Lead optimization and QSAR. Principles of Pharmacokinetics.
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