Medicinal Chemistry 1
A.Y. 2024/2025
Learning objectives
The course aims to provide the student with:
a) the knowledge that underlies the design and development of new active ingredients having the necessary requisites to be able to become drug candidates;
b) a good knowledge of the properties, the mechanisms of action and the use of the different classes of drugs treated;
c) the fundamental knowledge on the structure-activity relationships for the purpose of a more rational design aimed at a therapeutic effect free from contraindications and toxic effects;
d) indications concerning the synthetic methods used for the preparation of some of the drugs considered.
a) the knowledge that underlies the design and development of new active ingredients having the necessary requisites to be able to become drug candidates;
b) a good knowledge of the properties, the mechanisms of action and the use of the different classes of drugs treated;
c) the fundamental knowledge on the structure-activity relationships for the purpose of a more rational design aimed at a therapeutic effect free from contraindications and toxic effects;
d) indications concerning the synthetic methods used for the preparation of some of the drugs considered.
Expected learning outcomes
The student must demonstrate to have acquired what is foreseen by the educational objectives.
In particular, the student must demonstrate that he / she has acquired and understood:
a) the basic concepts of Medicinal Chemistry and the fundamental elements of drug design;
b) the notions provided on the chemical, chemical-physical, structural properties and on the mechanism of action of the drugs belonging to the therapeutic classes considered and the main synthetic strategies that can be used for the preparation of drugs.
In particular, the student must demonstrate that he / she has acquired and understood:
a) the basic concepts of Medicinal Chemistry and the fundamental elements of drug design;
b) the notions provided on the chemical, chemical-physical, structural properties and on the mechanism of action of the drugs belonging to the therapeutic classes considered and the main synthetic strategies that can be used for the preparation of drugs.
Lesson period: Activity scheduled over several sessions (see Course syllabus and organization section for more detailed information).
Assessment methods: Esame
Assessment result: voto verbalizzato in trentesimi
Single course
This course can be attended as a single course.
Course syllabus and organization
Linea AK
Responsible
Lesson period
year
Course syllabus
The syllabus is divided into two main parts: general and systematic parts.
General part:
Introduction to Medicinal Chemistry:
- Discovery and development of new drugs
- Molecular mechanisms of drug action
- Molecular targets of drugs
Drug design and development:
- Sources of research for lead compounds
- New "Drug design" strategies
- Structure-activity relationships (SAR).
- Pharmacophore research.
- Isosteria and bioisosteria
- Chemical-physical and biopharmaceutical properties of drugs and pharmacokinetics
- Prodrugs (prodrugs)
- Quantitative Relationships Structure-Activity (QSAR)
Systematic part:
- Antiseptics and disinfectants
- Synthetic antibacterials
- Antibiotics
- Antimycobacterial drugs
- Antiparasitic drugs
- Antimalarial drugs
- Anthelmintic drugs
- Antifungal drugs
- Antiviral drugs
- Anticancer drugs
- Steroid hormones (glucocorticoids, mineralocorticoids, estrogens, progestins and androgens) and related drugs
- Hypoglycemic drugs
General part:
Introduction to Medicinal Chemistry:
- Discovery and development of new drugs
- Molecular mechanisms of drug action
- Molecular targets of drugs
Drug design and development:
- Sources of research for lead compounds
- New "Drug design" strategies
- Structure-activity relationships (SAR).
- Pharmacophore research.
- Isosteria and bioisosteria
- Chemical-physical and biopharmaceutical properties of drugs and pharmacokinetics
- Prodrugs (prodrugs)
- Quantitative Relationships Structure-Activity (QSAR)
Systematic part:
- Antiseptics and disinfectants
- Synthetic antibacterials
- Antibiotics
- Antimycobacterial drugs
- Antiparasitic drugs
- Antimalarial drugs
- Anthelmintic drugs
- Antifungal drugs
- Antiviral drugs
- Anticancer drugs
- Steroid hormones (glucocorticoids, mineralocorticoids, estrogens, progestins and androgens) and related drugs
- Hypoglycemic drugs
Prerequisites for admission
In order to address the topics of the course, the student should have a good knowledge of organic chemistry, biological chemistry and a basic knowledge of physiology.
In addition to the prerequisites set out in the course study plan, the student should pass the Organic Chemistry II exam before this, in order to better understand the synthetic topics.
In addition to the prerequisites set out in the course study plan, the student should pass the Organic Chemistry II exam before this, in order to better understand the synthetic topics.
Teaching methods
The course includes lectures during which the syllabus topics are explained.
Teaching Resources
Recommended books:
Graham L. Patrick
Chimica Farmaceutica
EdiSES, Napoli
Thomas L. Lemke, David A. Williams
Foye's Principi di Chimica Farmaceutica
PICCIN, Padova
Alberto Gasco, Fulvio Gualtieri, Carlo Melchiorre
Chimica Farmaceutica - Seconda edizione
Zanichelli, Bologna
Supporting material:
Avaialble in digital format by download from Ariel site.
Graham L. Patrick
Chimica Farmaceutica
EdiSES, Napoli
Thomas L. Lemke, David A. Williams
Foye's Principi di Chimica Farmaceutica
PICCIN, Padova
Alberto Gasco, Fulvio Gualtieri, Carlo Melchiorre
Chimica Farmaceutica - Seconda edizione
Zanichelli, Bologna
Supporting material:
Avaialble in digital format by download from Ariel site.
Assessment methods and Criteria
The final exam is a written test of 30 questions (15 on the general part and 15 on the systematic part of drugs) which must be completed in 90 minutes. The overall evaluation is scored in thirtieths and, in particular, each question can be evaluated with a maximum of 1/30 for a total amount of 30/30. The final score of the exam is communicated by e-mail via the SIFA/UniMia platform within one week from the date of taking the written test, unless otherwise communicated. Examples of the written exam are available on the Ariel platform of the Course.
Furthermore, attending students have the opportunity to take the exam with two intermediate written tests: the first is scheduled for the end of January, while the second in June and, optionally, in September. Each test must be completed in 45 minutes and consists of 15 questions respectively on the program of the first and second semester. The overall evaluation is scored in thirtieths and, in particular, each question can be evaluated with a maximum of 2/30 for a total of 30/30. Only the student passing the first test with at least a score of 16/30 can access to the second test. If one of the two tests is not passed, the student must take the full exam (see above) or wait for the next academic year when the new intermediate test will be available. The final score is given by the average of the scores acquired in the two intermediate tests and, as for the full exam, is communicated by e-mail via the SIFA/UniMia platform within one week from the date of taking the written test, unless otherwise communicated.
Furthermore, attending students have the opportunity to take the exam with two intermediate written tests: the first is scheduled for the end of January, while the second in June and, optionally, in September. Each test must be completed in 45 minutes and consists of 15 questions respectively on the program of the first and second semester. The overall evaluation is scored in thirtieths and, in particular, each question can be evaluated with a maximum of 2/30 for a total of 30/30. Only the student passing the first test with at least a score of 16/30 can access to the second test. If one of the two tests is not passed, the student must take the full exam (see above) or wait for the next academic year when the new intermediate test will be available. The final score is given by the average of the scores acquired in the two intermediate tests and, as for the full exam, is communicated by e-mail via the SIFA/UniMia platform within one week from the date of taking the written test, unless otherwise communicated.
CHIM/08 - PHARMACEUTICAL CHEMISTRY - University credits: 10
Lessons: 80 hours
Professor:
Pedretti Alessandro
Shifts:
Turno
Professor:
Pedretti AlessandroLinea LZ
Responsible
Lesson period
year
Course syllabus
The programme is divided in two parts: General part and Systematic part.
General part
Introduction to Medicinal Chemistry:
- Discovery and development of new drugs
- Drug-target interaction
- Molecular targets of drugs: structural and transport proteins, enzymes, receptors, nucleic acids
Drug discovery, design and development:
- Identification of lead compounds
- "Drug design" strategies
- Structure-Activity Relationships (SAR)
- Pharmacophore search
- Isosteria and bioisosteria
- Stereoisomerism
- Pharmacokinetics of drugs: Absorption, Distribution, Metabolism, Elimination
- Prodrugs
Quantitative Structure-Activity Relationships (QSAR)
Systematic part
- Disinfectants and Antiseptics
- Synthetic antibacterials
- Antibiotics
- Antimycobacterial drugs
- Antiparasitic drugs
- Antifungal drugs
- Antiviral drugs
- Anticancer drugs
General part
Introduction to Medicinal Chemistry:
- Discovery and development of new drugs
- Drug-target interaction
- Molecular targets of drugs: structural and transport proteins, enzymes, receptors, nucleic acids
Drug discovery, design and development:
- Identification of lead compounds
- "Drug design" strategies
- Structure-Activity Relationships (SAR)
- Pharmacophore search
- Isosteria and bioisosteria
- Stereoisomerism
- Pharmacokinetics of drugs: Absorption, Distribution, Metabolism, Elimination
- Prodrugs
Quantitative Structure-Activity Relationships (QSAR)
Systematic part
- Disinfectants and Antiseptics
- Synthetic antibacterials
- Antibiotics
- Antimycobacterial drugs
- Antiparasitic drugs
- Antifungal drugs
- Antiviral drugs
- Anticancer drugs
Prerequisites for admission
To adequately address the contents of the course it is necessary to have a good knowledge of organic chemistry and biological chemistry. Therefore, in addition to the prerequisites set out in the course study plan, it is advisable to pass the Organic Chemistry II exam before this, in order to better understand the synthetic aspects.
Teaching methods
The course includes lectures during which the topics covered by the program will be illustrated and explained.
Teaching Resources
The teaching material shown during the lectures will be made available on the MyAriel platform.
Recommended books to support the topics covered in class:
1. G. L. Patrick: Chimica Farmaceutica, III Ed. EdiSES - Napoli (2015). ISBN: 978-88-7959-845-3.
2. FOYE'S: Principi di Chimica Farmaceutica, VII Ed. PICCIN (2021). ISBN: 978-88-299-3153-8.
3. FOYE'S: Principi di Chimica Farmaceutica: L'ESSENZIALE, PICCIN (2017). ISBN: 978-88-299-2867-5.
Recommended books to support the topics covered in class:
1. G. L. Patrick: Chimica Farmaceutica, III Ed. EdiSES - Napoli (2015). ISBN: 978-88-7959-845-3.
2. FOYE'S: Principi di Chimica Farmaceutica, VII Ed. PICCIN (2021). ISBN: 978-88-299-3153-8.
3. FOYE'S: Principi di Chimica Farmaceutica: L'ESSENZIALE, PICCIN (2017). ISBN: 978-88-299-2867-5.
Assessment methods and Criteria
LEARNING VERIFICATION
The exam consists of a written test lasting 90 minutes. It is articulated in closed and open questions related to the topics covered in class.
EVALUATION CRITERIA
The evaluation will be carried out considering the ability to correctly understand the questions and to choose, elaborate and connect the knowledge acquired during the course, using an appropriate scientific language.
In particular, the learning assessment is evaluated by a mark out of thirty with a minimum grade of 18/30.
The exam consists of a written test lasting 90 minutes. It is articulated in closed and open questions related to the topics covered in class.
EVALUATION CRITERIA
The evaluation will be carried out considering the ability to correctly understand the questions and to choose, elaborate and connect the knowledge acquired during the course, using an appropriate scientific language.
In particular, the learning assessment is evaluated by a mark out of thirty with a minimum grade of 18/30.
CHIM/08 - PHARMACEUTICAL CHEMISTRY - University credits: 10
Lessons: 80 hours
Professor:
Dallanoce Clelia Mariangiola Luisa
Shifts:
Turno
Professor:
Dallanoce Clelia Mariangiola LuisaEducational website(s)
Professor(s)
Reception:
By appointment
Reception:
Every day by appointment
Deparment of Pharmaceutical Sciences - Medicinal Chemistry