The course is finalized to examine the problems encountered and the strategies adopted to obtain a new drug. To achieve this aim, general information and specific examples will be given, considering the various steps that, starting from an original idea, lead to the realization of a new therapeutic agent, the approval of the drug and the marketing of the medicinal product that contains it. 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, which constitutes relevant aspects within the reference degree.

1. Research phase

2. Non-clinical development phase

3. Clinical development phase

4. Strategies and approaches to optimize investments

5. The patent

6. Nomenclature and classification of drugs: preparatory and integrative aspects

7. Computerized and paper bibliographic research aimed to acquiring evaluation elements for a better design analysis: secondary and primary sources

8. Identification strategies for new hit and lead compounds

9. Combinatorial chemistry: characteristics and applications

10. Primary exploration of structure-activity relationships (SAR)

11. Prodrugs

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 drug design and development. Through the expertise acquired the student will be able to develop critical skills, independence of judgment and communication skills that allow him/her 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

On specific topics, thematic in-depth studies will be carried out and, if necessary, tutoring and remedial activities may be provided.

Teaching

Frontal lessons possibly supplemented by brief presentations on specific issues [when the topics of the program and the situations allow it, innovative teaching elements that refer to techniques, such as problem-based learning (PBL) or debate may be applied]. 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: material supplied during the course.

Support sources: scientific articles commented during the course.

Consultation sources: a) material available through computerized and paper bibliographic research; b) Wermuth CG, The practice of medicinal chemistry Elsevier Academic Press 2004.

Assessment

Oral exam, integrated with Medicinal chemistry II, after a written test (unless otherwise indicated depending to the health emergency).

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 part of test related to Drug design and development will include 2 MCQ, 2 TFQ and 2 QOR, and 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 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 exam, but if a negative result of the second written test 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 due to the fact that this course has a higher number of ECTS.

Finally, some advices 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.

Disabilità e DSA

Le studentesse e gli studenti che hanno registrato la certificazione di disabilità o la certificazione di DSA presso l'Ufficio Inclusione e diritto allo studio, possono chiedere di utilizzare le mappe concettuali (per parole chiave) durante la prova di esame.

A tal fine, è necessario inviare le mappe, due settimane prima dell’appello di esame, alla o al docente del corso, che ne verificherà la coerenza con le indicazioni delle linee guida di ateneo e potrà chiederne la modifica.

Attendance

Same as for the attending students.

Course books

Same as for the attending students.

Assessment

Same as for the attending students.

Disabilità e DSA

Le studentesse e gli studenti che hanno registrato la certificazione di disabilità o la certificazione di DSA presso l'Ufficio Inclusione e diritto allo studio, possono chiedere di utilizzare le mappe concettuali (per parole chiave) durante la prova di esame.

A tal fine, è necessario inviare le mappe, due settimane prima dell’appello di esame, alla o al docente del corso, che ne verificherà la coerenza con le indicazioni delle linee guida di ateneo e potrà chiederne la modifica.