The main goal of this module is to provide key insights on the chemistry of selected drug classes. This is a fundamental part of the background knowledge we aim at providing to future pharmacists and, more in general, healthcare professionals.

For each drug class, therapeutic opportunities are described in details and linked to chemical structures.

Key molecules and detailed structure-activity relationships are discussed. When relevant, the incentives and the strategies that, from first-generation molecules, led to more advanced compounds are discussed.

Part 1

• Adrenergic Drugs
• Antisecretory Drugs
• Heart Medications
  • Heart Failure Drugs
  • Antiarithmic Drugs
  • Treatment of Angina Pectoris and Ischaemic Heart Disease
• Antihypertensive Drugs
• Diuretics
• Antithrombotic Agents
• Hypolipidemic agents

Part 2

• Drugs Acting on Nuclear Receptors
  • Estrogens
  • Progestinics
  • Androgens
• Treatment of Erectile Disfunction 
• Antihyperglycemic Agents
• Antineoplastic

Part 3

Introduction to Antimicrobial Agents

• Antibiotics
  • Molecules Interfering with the Biosynthesis of the Cell Wall
  • Molecules Interfering with Protein Synthesis 
• Antibacterial Chemotherapy
• Antiviral Chemotherapy
• Antiprotozoal Agents 
• Antifungal Agents

Medicinal Chemistry I

Knowledge and Understanding: starting either from the structure of a compound or from the structure and a minimal set of notions, interpret and discuss activity, structure-activty relationship, elements of bioavailability and matabolism. Develop a detailed understanding of how, within a drug class, initial prototypes evolve into more advanced drugs

Applied Knowledge and Understanding: how the aforementioned general approach applies to specific drug classes. Notable examples will be discussed in details as case studies.  

Making Judgements: master the idea that drug development implies a constant trade-off between multiple, often conflicting, instances. This element is explained resorting to case studies

Communication Skills: master the correct terminology (standard of practise- or IUPAC-compliant) to correctly address structures and SARs 

Learning Skills: ideally, by the end of the module, the student should be able to apply the notions and the methods learned to molecules that, while belonging to drug classes they are familiar with, they have never seen before.

The teaching material prepared by the lecturer in addition to recommended textbooks (such as for instance slides, lecture notes, exercises, bibliography) and communications from the lecturer specific to the course can be found inside the Moodle platform › blended.uniurb.it

None

Teaching

Frontal Lessons

Attendance

Attendance is strongly encouraged yet not mandatory

Course books

Textbook: 

• Gasco, Chimica Farmaceutica, CEA

For the exam:

• Slides and course work provided

Extra/For Consultation:

• Foye, Priciples of Medicinal Chemistry (any recent edition)
• Goodman & Gilman, The Pharmacological Basis of Therapeutics (any recent edition)
• Clementi & Fumagalli, Farmacologia Generale e Molecolare, EDRA (available in Italian only, to the best of my knowledge)
• Silverman, The Organic Chemistry of DRug Design and Drug Action, Elsevier

Assessment

Written and oral exam

The final exam of this module has two parts: a written and an oral assessment. There are no differences in terms of contents or format. In both cases, the students will have to answer the equivalent of open frame questions, in writing in one case, orally in the other one. Combining a written assessment with an oral one makes it possible to test each student thoruoghly yet efficiently, considering the average size of each cohort and the remarkable breadth of this module's programme.

A 17/30 mark in the written test is necessary to be admitted to the oral assessment.

The mark obtained in the written exam is only valid for that specific round (appello).

Since the final mark is obtained averaging marks from both written and oral assessments, the oral exam is always mandatory, regardless of the mark obtained in the written part (i.e., even a very high mark in the written test does not guarantee to pass the overall exam neither does it allow the candidate to skip the oral exam) 

Midterm assessments (Parziali)

Please read very carefully.

Students attending for the first time Year 4 in AA 2024/25 (based on official records) are given a strictly one-time possibility to take two midterm written tests in early November 2024 on Part 1 (see above) of the module's program and on mid-December 2024 on Part 2 (see above) of the module's program.

Students obtaining a mark of 17/30 or better on both tests will have a one-time opportunity to be tested in one round (appello) of their choice during the winter exam session (January/February 2025), with questions in both the written and the oral assessments only convering Part 3 of the program. The final mark will be obtained averaging midterms, final written and oral assessments.

Interpretation of the Final Mark

27/30 - 30/30 cum laude. The candidate correctly understands the relationship that exists between the physico-chemical profile of a drug, the SAR and, when known, the target-molecule interactions. All chemistry-related aspects are discussed in details, using proper terminology, showing a sound command of relevant aspects of organic chemistry. The link between structure and mechanism of action is clearly understood. The candidate can recognise the drug classes and the notable molecules discussed in the module. The candidate can discuss proficiently the simple synthetic routes discussed in the module. 

24/30 - 26/30. The candidate understands fairly well the relationship that exists between the physico-chemical profile of a drug, the SAR and, when known, the target-molecule interactions. Chemistry-related aspects are almost always discussed using proper (IUPAC-compliant) terminology and relevant aspects of organic chemistry are connected fairly well with presented molecules. The link between structure and mechanism of action is usually understood. The candidate can recognise drug classes if not notable molecules discussed in the module.

21/30 - 23/30. The candidate understands at least key elements of the relationship that exists between the physico-chemical profile of a drug, the SAR and, when known, the target-molecule interactions. Aspects of organic chemistry related to the presented molecules can be partially discussed even if not always using the most proper terminology. The link between structure and mechanism of action is not always understood. The candidate can recognise key drug classes discussed in the module.

18/30 - 20/30. The candidate can only name some elements of the relationship that exists between the physico-chemical profile of a drug, the SAR and, when known, the target-molecule interactions. The understanding of chemistry-related aspects is shallow. The link between structure and mechanism of action is only partially understood. The candidate can only recognise some of the drug classes discussed in the module.

Disability and Specific Learning Disorders (SLD)

Students who have registered their disability certification or SLD certification with the Inclusion and Right to Study Office can request to use conceptual maps (for keywords) during exams.

To this end, it is necessary to send the maps, two weeks before the exam date, to the course instructor, who will verify their compliance with the university guidelines and may request modifications.

Teaching

No difference for non-attending students. Note: attendance is strongly encouraged

Attendance

No difference for non-attending students. Note: attendance is strongly encouraged

Course books

Non-attending students might find particularly useful the following chapters from Foye's Principles of Medicinal Chemistry (any recent edition will do):

Ch 16-19

Ch 20-21

Ch 24

Ch 29-33 

Assessment

No difference for non-attending students. Note: attendance is strongly encouraged

Disability and Specific Learning Disorders (SLD)

Students who have registered their disability certification or SLD certification with the Inclusion and Right to Study Office can request to use conceptual maps (for keywords) during exams.

To this end, it is necessary to send the maps, two weeks before the exam date, to the course instructor, who will verify their compliance with the university guidelines and may request modifications.

Antineoplastic drugs have been included in the program starting from the academic year 2024/25.

Until the end of the academic year 2024/25, this topic will not be part of the material to be presented in the exam for those who attended the course previously.

Starting from the academic year 2025/26, the topic will be part of the exam program for everyone.