Medicinal Chemistry 2
A.Y. 2025/2026
Learning objectives
The course aims at providing the most relevant concepts related to the design, synthesis, physico-chemical and stereo-electronic properties, mechanism of action, therapeutic application and side effects of the drugs belonging to the investigated classes. In particular, lectures will deal with the structure-activity relationships and the approaches applied in medicinal chemistry to optimize the pharmacodynamic profile and the pharmacokinetic properties of drugs. Based on the fundamentals acquired in the course of Medicinal and Toxicological Chemistry 1, in the present course the student should accomplish a good overall background in medicinal chemistry, through the study of drugs acting on the central and peripheral nervous system, the cardiovascular and anti-histamine drugs, the non-steroidal anti-inflammatory agents.
Expected learning outcomes
Expected learning outcomes (nuovo testo da inserire in W4)
Knowledge and understanding. The course aims to ascertaining the student's knowledge of the approaches and methods presented during the lectures, particularly those related to the structural aspects of drugs, their genesis and their therapeutic classification.
Applying knowledge and understanding. During the exam, the student should be able to apply knowledge and understanding, in particular by appropriately discussing the main aspects of the structure/synthesis of the main compounds of a class of drugs, together with their related therapeutic utility.
Making judgements. The student will answer any question with pertinence and criticism, both in the written and oral part of the exam. In their answers, students are frequently requested to motivate their own choices.
Communication. During the exam, the student will demonstrate to explain and develop concepts with clarity, synthesis and language skills. Clarity of presentation and communication skills are part of the overall evaluation.
Lifelong learning skills. The main objective of the course is that to ascertain the strengthening of the student's background in Medicinal Chemistry: the acquired competence will help the student's informed choice (professionalizing courses/thesis lab) towards completing the educational path.
Knowledge and understanding. The course aims to ascertaining the student's knowledge of the approaches and methods presented during the lectures, particularly those related to the structural aspects of drugs, their genesis and their therapeutic classification.
Applying knowledge and understanding. During the exam, the student should be able to apply knowledge and understanding, in particular by appropriately discussing the main aspects of the structure/synthesis of the main compounds of a class of drugs, together with their related therapeutic utility.
Making judgements. The student will answer any question with pertinence and criticism, both in the written and oral part of the exam. In their answers, students are frequently requested to motivate their own choices.
Communication. During the exam, the student will demonstrate to explain and develop concepts with clarity, synthesis and language skills. Clarity of presentation and communication skills are part of the overall evaluation.
Lifelong learning skills. The main objective of the course is that to ascertain the strengthening of the student's background in Medicinal Chemistry: the acquired competence will help the student's informed choice (professionalizing courses/thesis lab) towards completing the educational path.
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 cannot be attended as a single course. Please check our list of single courses to find the ones available for enrolment.
Course syllabus and organization
Linea AK
Responsible
Lesson period
year
Course syllabus
The course is structured as lectures totaling 10 academic credits.
The course program focuses on the study of biomolecular processes involving neurotransmitters, neuromodulators, and second messengers, as well as the structural characteristics (stereo-electronic requirements, topology, topography, conformational equilibria, acid-base properties) of drugs (ligands) that interact with major biological targets (receptors, enzymes, ion channels).
The pharmaceutical-chemical aspects covered include the study of structural modifications of biologically active natural compounds, the impact of molecular fragment variations in lead compounds on affinity, activity, selectivity, and bioavailability profiles, the discussion of synthetic strategies for major active pharmaceutical ingredients, and the relevance of new insights into drug mechanisms of action for therapeutic use.
Based on these general principles, the course illustrates and discusses drugs acting at the following levels:
a) Drugs affecting parasympathetic neurotransmission (agents acting on nicotinic and muscarinic receptors, cholinesterase inhibitors) and sympathetic neurotransmission (agents acting on alpha and beta adrenergic receptors, MAO and COMT inhibitors).
b) Drugs acting on the central nervous system (anesthetics, anxiolytics and hypnotic-sedatives, anticonvulsants, antiparkinsonian agents, opioid analgesics, antipsychotics, antidepressants, hallucinogens, and related substances of abuse).
c) Cardiovascular drugs (cardiotonic glycosides, antianginal agents, antiarrhythmics, calcium channel blockers, potassium channel activators, ACE inhibitors, angiotensin antagonists, diuretics).
d) Non-steroidal anti-inflammatory drugs (NSAIDs).
e) Antihistaminic agents, antiallergic agents, and antiulcer drugs.
The course program focuses on the study of biomolecular processes involving neurotransmitters, neuromodulators, and second messengers, as well as the structural characteristics (stereo-electronic requirements, topology, topography, conformational equilibria, acid-base properties) of drugs (ligands) that interact with major biological targets (receptors, enzymes, ion channels).
The pharmaceutical-chemical aspects covered include the study of structural modifications of biologically active natural compounds, the impact of molecular fragment variations in lead compounds on affinity, activity, selectivity, and bioavailability profiles, the discussion of synthetic strategies for major active pharmaceutical ingredients, and the relevance of new insights into drug mechanisms of action for therapeutic use.
Based on these general principles, the course illustrates and discusses drugs acting at the following levels:
a) Drugs affecting parasympathetic neurotransmission (agents acting on nicotinic and muscarinic receptors, cholinesterase inhibitors) and sympathetic neurotransmission (agents acting on alpha and beta adrenergic receptors, MAO and COMT inhibitors).
b) Drugs acting on the central nervous system (anesthetics, anxiolytics and hypnotic-sedatives, anticonvulsants, antiparkinsonian agents, opioid analgesics, antipsychotics, antidepressants, hallucinogens, and related substances of abuse).
c) Cardiovascular drugs (cardiotonic glycosides, antianginal agents, antiarrhythmics, calcium channel blockers, potassium channel activators, ACE inhibitors, angiotensin antagonists, diuretics).
d) Non-steroidal anti-inflammatory drugs (NSAIDs).
e) Antihistaminic agents, antiallergic agents, and antiulcer drugs.
Prerequisites for admission
For a fruitful participation in the lessons, which take place throughout the academic year, students should have acquired the knowledge from the courses in Organic Chemistry and Medicinal and Toxicological Chemistry I. In order to take the exam, students must have passed the exams in Medicinal and Toxicological Chemistry I and Organic Chemistry II.
Teaching methods
The teaching method consists of lectures totaling 10 academic credits (80 hours).
Teaching Resources
The slides presented in the classroom are available as pdf files on the myAriel website of the course.
For a further deepening of the topics, the following textbooks are recommended.
A) T. L. Lemke, D. A. Williams: "Foye's Principi di Chimica Farmaceutica", Piccin - Nuova Libraria Editore, 7a edizione italiana (2014).
B) G. L. Patrick: "Introduzione alla Chimica Farmaceutica", EdiSES, edizione integrata (2015).
C) "Chimica Farmaceutica", 2a edizione italiana, A. Gasco, F. Gualtieri, C. Melchiorre Editori, Casa Editrice Ambrosiana (2019).
D) "Goodman & Gilman's. The Pharmacological Basis of Therapeutics" Thirteenth Edition, McGraw-Hill Education (2018).
E) "Farmacologia Generale e Molecolare", F. Clementi, G. Fumagalli Editori, 4a edizione, EDRA (2016).
For a further deepening of the topics, the following textbooks are recommended.
A) T. L. Lemke, D. A. Williams: "Foye's Principi di Chimica Farmaceutica", Piccin - Nuova Libraria Editore, 7a edizione italiana (2014).
B) G. L. Patrick: "Introduzione alla Chimica Farmaceutica", EdiSES, edizione integrata (2015).
C) "Chimica Farmaceutica", 2a edizione italiana, A. Gasco, F. Gualtieri, C. Melchiorre Editori, Casa Editrice Ambrosiana (2019).
D) "Goodman & Gilman's. The Pharmacological Basis of Therapeutics" Thirteenth Edition, McGraw-Hill Education (2018).
E) "Farmacologia Generale e Molecolare", F. Clementi, G. Fumagalli Editori, 4a edizione, EDRA (2016).
Assessment methods and Criteria
Students who attend classes for the entire duration of the course have the opportunity to take two written midterm exams (each lasting approximately 2.5 hours), subject to verification of attendance. These exams are held in February and July and cover the course content of the first and second semesters, respectively. Each exam typically consists of three open-ended questions.
The questions require students to comment on drug structures (either provided in the exam or requested from the student), illustrating the mechanism of action, therapeutic class, and side effects, as well as discussing structure-activity relationships, physicochemical properties, and synthetic approaches.
Assessment is based on the student's ability to organize responses to all questions, the quality and clarity of the answers, and the appropriate use of scientific language. To pass the exam through this method, the student must achieve a passing grade in both midterms. The final grade (out of 30) is the average of the two scores. No oral integration is foreseen for this exam format.
The exam grade can only be recorded after passing the exams in Medicinal and Toxicological Chemistry I and Organic Chemistry II.
The standard exam session consists of a written test (approximately 2.5 hours), typically including three open-ended questions, following the same format as the midterm exams. To pass the written test, the student must provide satisfactory answers to at least two of the three questions. The final score for the written test is based on an overall evaluation of the entire paper.
Students who pass the written test proceed to the oral exam, during which the written test is reviewed and discussed, and an average of two to three additional questions are asked, covering the entire course syllabus. The final grade, expressed out of 30, is primarily determined by the written test score.
For standard exam sessions, the results of the written test are usually communicated within two weeks, along with feedback and corrections, prior to the oral exam. Students who do not pass the written test must retake the exam and may register for the next session without restrictions. There are at least six exam sessions per year, scheduled according to the calendar set by the Faculty of Pharmaceutical Sciences.
The questions require students to comment on drug structures (either provided in the exam or requested from the student), illustrating the mechanism of action, therapeutic class, and side effects, as well as discussing structure-activity relationships, physicochemical properties, and synthetic approaches.
Assessment is based on the student's ability to organize responses to all questions, the quality and clarity of the answers, and the appropriate use of scientific language. To pass the exam through this method, the student must achieve a passing grade in both midterms. The final grade (out of 30) is the average of the two scores. No oral integration is foreseen for this exam format.
The exam grade can only be recorded after passing the exams in Medicinal and Toxicological Chemistry I and Organic Chemistry II.
The standard exam session consists of a written test (approximately 2.5 hours), typically including three open-ended questions, following the same format as the midterm exams. To pass the written test, the student must provide satisfactory answers to at least two of the three questions. The final score for the written test is based on an overall evaluation of the entire paper.
Students who pass the written test proceed to the oral exam, during which the written test is reviewed and discussed, and an average of two to three additional questions are asked, covering the entire course syllabus. The final grade, expressed out of 30, is primarily determined by the written test score.
For standard exam sessions, the results of the written test are usually communicated within two weeks, along with feedback and corrections, prior to the oral exam. Students who do not pass the written test must retake the exam and may register for the next session without restrictions. There are at least six exam sessions per year, scheduled according to the calendar set by the Faculty of Pharmaceutical Sciences.
CHIM/08 - PHARMACEUTICAL CHEMISTRY - University credits: 10
Lessons: 80 hours
Professor:
Tamborini Lucia
Linea LZ
Responsible
Lesson period
year
CHIM/08 - PHARMACEUTICAL CHEMISTRY - University credits: 10
Lessons: 80 hours
Professor:
Pallavicini Marco
Professor(s)