Unit MEDICINAL CHEMISTRY III
- Course
- Industrial pharmacy
- Study-unit Code
- 65003906
- Curriculum
- In all curricula
- Teacher
- Antimo Gioiello
- Teachers
-
- Antimo Gioiello
- Andrea Carotti (Codocenza)
- Hours
- 40 ore - Antimo Gioiello
- 15 ore (Codocenza) - Andrea Carotti
- CFU
- 6
- Course Regulation
- Coorte 2023
- Offered
- 2026/27
- Learning activities
- Caratterizzante
- Area
- Discipline farmaceutico-alimentari
- Sector
- 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, approaches, and technologies leading to the discovery and development of novel drugs with insights into the key steps that allow its completion. A particular attention will be devoted to strategies and technologies enabling innovation and sustainability in medicinal chemistry.
- 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 aim of the course of Medicinal Chemistry III is to provide students with a broad understanding of the drug discovery and development process. Particular attention will be devoted to innovative approaches and emerging technologies that characterize the evolution of medicinal chemistry and the modernization of the pharmaceutical industry.
The main knowledge acquired during the course will include:
Analysis of the different stages involved in the discovery and development of a new drug
Design and synthesis of chemical libraries based on the concepts of molecular diversity and complexity, lead-likeness and drug-likeness, as well as on sources and compounds of natural origin
Approaches for the discovery, optimization, and development of lead compounds
Computational methods for studying ligand/biological target interactions
Enabling chemical technologies applied to medicinal chemistry
The main skills expected to be acquired by the end of the course will include:
Ability to design experimental studies aimed at discovering new hit compounds, lead compounds, and clinical candidates
Ability to analyze drug development processes in order to identify potential critical issues and perform risk assessments
Ability to design and synthesize chemical libraries
Ability to apply ligand/protein interaction studies and design structural modifications of hit and lead compounds. - 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)
- Organic Chemistry (I and II)
- Pharmacology
Skills which the student must have at the beginning of the course:
- Laboratory of drug extraction and synthesis
- English
Useful knowledge that a student must possess at the beginning of the course:
- General chemistry
- Physical chemistry - Teaching methods
- - Frontal lectures on all topics of the course.
- Seminars on topics of general interest as well as based on technological and methodological innovation.
- Computational chemistry practice will also be provided. - Other information
- The supplementary and workshop/seminar activities are determined in agreement with students. They may cover seminars, technical and practical discussions, and reinterpretations of common laboratory practices.
- Learning verification modality
- The exam includes an oral exam consisting of a discussion 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.
For information on support services for students with disabilities see: http://www.unipg.it/disabilita-e-dsa - Extended program
- Introduction
Selection and validation of a biological target
Primary and secondary screenings
Computational chemistry
- Virtual screening
- Target- and ligand-based approaches
- Chemoinformatics (COMFA, AI)
Hit-to-lead optimization
- 'Traditional' and ‘fragment-based’ approach in medicinal chemistry
- Property and activity of hit and lead compounds
- Strategies for the discovery and development of a lead compound
- Strategies for compounds libraries building (drug-like, lead-like, natural-like)
Identification of lead compounds
Importance of synthesis in drug discovery
- Concepts
- Sustainable drug discovery and green chemistry principles
- Case studies
Combinatorial and solid phase synthesis
- Principles and metods
- Antisense oligonucleotides
- Examples and applications
- Parallel synthesis and split-and-pool approach
Target- e diversity-oriented synthesis
- Principles and applications in drug discovery
- DOS libraries (es: shikimic acid)
- Biomimetic DOS (es: galantanamine)
Complexity generating reactions
- Chemical diversity and complexity
- Tandem and multicomponent reactions
Microwave and continuous flow synthesis
- Principles and tools
- Porcess optimization and DoE
- Examples and applications
Photo- and electro-chemistry
- Principles, history and tools
- Examples and applications
Biocatalysis in drug synthesis
- Principles and tools
- Examples and applications - Obiettivi Agenda 2030 per lo sviluppo sostenibile
- Yes