Unit MEDICINAL CHEMISTRY III
- Course
- Chemistry and technology of drugs
- Study-unit Code
- 65003906
- Location
- PERUGIA
- Curriculum
- In all curricula
- Teacher
- Antonio Macchiarulo
- Teachers
-
- Antonio Macchiarulo
- Hours
- 48 ore - Antonio Macchiarulo
- CFU
- 6
- Course Regulation
- Coorte 2016
- Offered
- 2020/21
- Learning activities
- Caratterizzante
- Area
- Discipline chimiche, farmaceutiche e tecnologiche
- Academic discipline
- CHIM/08
- Type of study-unit
- Obbligatorio (Required)
- Type of learning activities
- Attività formativa monodisciplinare
- Language of instruction
- Italian
- Contents
- Provide a broad knowledge on the process of drug discovery with insights on key steps that allow its successful completion.
- Reference texts
- 1) Introduzione alla Chimica Farmaceutica, Graham L. Patrick, II Edizione (Editore: EdiSes).
2) Drugs: From Discovery to Approval, 2nd Edition Rick Ng (Editore: Wiley-Blackwell). - Educational objectives
- The overall aim of the course is to provide the student a wide knowledge on the process of drug discovery with insights on key steps that allow its successful completion.
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. - 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:
- Medicinal Chemistry (I and II); Pharmacology, pharmacognosy and toxicology general; Animal and plant biology.
Skills which the student must have at the beginning of the course:
- Organic Chemistry (I and II); Physiology; English.
Useful knowledge that a student must possess at the beginning of the course:
- Mathematics (statistics); Physical chemistry. - 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. - Extended program
- Definition and evolution of the process of drug discovery. Methods for identification and validation of a biological target. Experimental and computational approaches to the acquisition of information about the function of a biological target. Traditional and large scale (HTS) biological assays. Definition and discovery of a "Lead compound". Combinatorial chemistry and construction of libraries of chemical compounds. Method of optimization of a "Lead compound". Representation of the molecular structure of a compound of biological interest and its mathematical description. Concept of chemical space and instruments for its exploration. Study of the interactions of a compound of biological interest with its target. Development of predictive models of biological activity (SAR, QSAR).