The course is finalized to examine the structure-activity relationships of drugs belonging to the therapeutic classes included in the program and it will consider mechanisms of action also; in some cases, it will be analyzed the influence that specific portions of the drug exert on the metabolism and toxicity. To achieve this aim, sometimes it will be also sometimes evaluated how drug design and optimization allow to improve the pharmacodynamic and pharmacokinetic profile. The contents of the course will be faced in a critical and interactive way with the additional aim of imparting and making acquire an analytical ability on the subjects, that constitutes relevant aspects within the reference degree.

1. Cardiac drugs

2. Diuretics

3. Hypotensives

4. Sympatholytics and vasodilators

5. Hypolipidemics

6. Antithrombotics

7. Anti-asthma and related drugs

8. Insulin and hypoglicemic drugs

  9. Thyroid drugs

10. Antiulcer and antiacids

11. Introduction to anti-infective drugs

12. Antibiotics

13. Antibacterials

14. Antimycobacterials

15. Antifungins

16. Antiprotozoals

17. Antivirals

18. Anthelmintics

Medicinal Chemistry I.

At the end of the formative activity related to the discipline, the student is supposed to know and understand the problems related to the studies finalized to the construction of the structure-activity relationships and the mechanism of action of the main examined classes and drugs; where appropriate also with regard to the aspects related to design (discovery, optimization...), metabolism and toxicity. Through the expertise acquired the student will be able to develop critical skills, independence of judgment and communication skills that allow him to produce reasoning on the topics covered. This scenario will also be developed through logical relationships and interactive discussions, which could be supported by the analysis of studies published in scientific journals relevant to teaching.

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

No teaching support activities are planned.

Teaching

Frontal lessons possibly supplemented by brief presentations on specific issues. Normally, on a weekly basis, exercises will be carried out on the topics covered, based on the contents of the written tests previously assigned.

Attendance

Attendance to classes is not mandatory but is strongly recommended on a regular basis to encourage both classroom interaction and the acquisition of knowledge and skills. Knowledge on organic chemistry and medicinal chemistry.

Course books

Primary source: Gasco A Gualtieri F Melchiorre C, Chimica farmaceutica I or II Ed. Casa Editrice Ambrosiana, 2015 or 2020 [Cap. 16-21, 22(5), 24, 25, 28(5), 30(3), 31, 33, 35-38, 39(2), 40, 41(2)] or Lemke TL, Williams DA Foye's Principles of medicinal chemistry VII Ed. Lippincott Williams & Wilkins 2013 [Cap. 21-29, 32(2), 33, 34(5,6), 35, 36, 38, 39].

Consultation sources: a) Patrick GL, An introduction to medicinal chemistry VI Ed. Oxford 2017; b) Beale JM Jr Block JH, Wilson and Gisvold’s Textbook of Organic, Medicinal and Pharmaceutical Chemistry XII Ed. Lippincott Williams & Wilkins 2011.

Assessment

Oral exam integrated with Drug design and development, and after a written test.

The written test, with the aim of producing a complete evaluation framework, is made of structured tests [multiple choice quizzes (MCQ), true/false quizzes (TFQ)] and unstructured tests [questions open response (QOR)]. It will thus be possible to establish, in a uniform way for all students, the level of knowledge achieved and whether the ability to use the acquired knowledge and concepts has been developed both to identify and use the theoretical and methodological approaches of the discipline and to realize the best application strategies related to specific problems. The test will include 4 MCQ, 5 TFQ and 4 QRO, and it will be evaluated according to the following scores. MCQ: exact 2, incorrect -1, not given: 0; TFQ: exact 0.4, incorrect -0.2, not given: 0; QOR: up to 5. The duration of the overall written test is quantifiable in 2 hours.

The oral exam will check the ability to use both knowledge and concepts to reason on the topics of the course, both to check the communication skills and to know the student is able to produce correlations between topics covered by the exam program. The oral exam, preceded by a comment on the written test, approximately lasts about 30 minutes.

Both the written test and the oral examination will be evaluated with a score expressed in thirtieths. The final grade will result from the oral exam, taking into consideration the outcome of the written test also. The student will be awarded an additional bonus point to the final teaching grade for each in-depth thematic presentation lasting at least 20 minutes.

The student can opt to support the tests of the two teachings at different times; in this case the written test will last 1 hour, and it will be made up of 2 MCQ, 3 TFQ, 2 QOR; the second test will have to be taken within two months or slightly later according to the calendar of the first useful call. The student can also take two written tests and a single oral exam after the second written test, but if a negative result of the second written test or the oral exam occurs, the first written test must be taken again. If the student chooses to take the test at two different times, the final grade will consist of the average of the two intermediate grades, possibly rounded according to the grade of Medicinal Chemistry II, since this course has a higher number of ECTS.

Finally, some advice to optimize the study. Since the programs of the two teachings are carried out in such a way as to establish correlations between the topics, it is strongly recommended to study both subjects and then subsequently evaluate whether to opt for the tests at different times. In any case, the advice is to initially study the topics from a general point of view and then go into detail. At the same time, while keeping the student in the program of his year of attendance, to rationalize the study it is advisable to update the material with what refers to the last year in which the lessons were carried out.

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.

Attendance

Same as for the attending students.

Course books

Same as for the attending students.

Assessment

Same as for the attending students.

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.