PHARMACEUTICAL AND TOXICOLOGICAL CHEMISTRY I
Academic year and teacher
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- Versione italiana
- Academic year
- 2022/2023
- Teacher
- SILVIA VERTUANI
- Credits
- 9
- Didactic period
- Primo Semestre
- SSD
- CHIM/08
Training objectives
- The course is integrated with the next course of Pharmaceutical Chemistry II. The main objective of the course is to provide students with basic informations to learn about the various classes of drugs today in therapy, with a classification based on therapeutic groups as well as on chemical class of substances.
The objective of the first part of the course is the knowledge of the nature of the interactions of drugs and their biological counterparts, the significance of receptor and biosisotery. Importance of prodrugs. Knowledge of enzymes which are substrates of drugs considered in the course.
The objective of the special part is knowledge of the different classes of anti-infective drugs, anti-cancer drugs, steroid hormones, anti-inflammatory steroid-like structures and non-steroidal anti-inflammatory, anticoagulants, anti-platelet aggregation and anti-lipemic drugs. Prerequisites
- The knowledge of basic Organic Chemistry, Biochemistry, Microbiology and Physiology is essential.
To take the final examination (learning assessment procedures), students must have passed the exam of Organic chemistry. Course programme
- General Introduction. Chemistry and drugs. The discovery of drugs. Stereochemistry and biological activity. Sterochemistry and drug activity: chirality, geometric isomers, conformational isomers. Stereochemistry of drugs and metabolism. Bioisostery. Classical and nonclassical bioisosters. Examples of bioisosteric analogs.Prodrugs. General aspects. Examples of prodrugs.Enzymes. Brief introduction on enzymes as catalysts, mechanism of enzyme catalysis. Drugs as inhibitors of enzymes.Second PartAntibacterial antibiotics. General aspects and classification. ß-Lactam antibiotics: penicillins, carbapenems, cephalosporins, monobactams. Macrolide antibiotics, polyenes and antifungal antibiotics. Polypeptides. Aminoglycoside antibiotics. Tetratracyclins. Phosphonates.Antibacterial Chemotherapeutics. Sulfonamides and quinolones as antibacterial agents. Nitrofurans and nitroimidazoles. Dihydrofolate reductase inhibitors.Antiprotozoal agents. Chincona alkaloids and analogs. Sulfamides and sulfones. Antibiotics as amebicides. Antitumor drugs. DNA-interacting drugs. DNA alkylators. Antimetabolites. DNA intercalators and active on topoisomerase, complexes of platinum and Drugs acting on tubulin / microtubule system, inhibitors of protein kinase. Antiviral Agents. Pyrimidine and purine nucleosides and nucleotides and structural analogs. Drugs active on DNA and RNA viruses. Drugs anti-retro viruses. Steroids hormones. Estrogens, progestins, androgens, glucocorticoids and mineralcorticoids.
Non-steroidal anti-inflammatory drugs.
Definition of NSAID, mechanism of action of NSAIDs, non selective COX1 NSAID selective COX2 inhibitors. Salicylic, anilinic, antranilic, arylalkanoic, oxicam drugs and various structures. Didactic methods
- Frontal lessons supported by presentations (ppt or precious) with diagrams, concept maps, illustrations taken from scientific articles;
classroom activities with active student participation (initial knowledge assessment, self-assessment tests, etc.).
Resources: teaching material presented in class, concept maps, supplementary material with links to websites, videos and animations, 3D molecules.
Classroom frontal lessons with computer support (slides and films) Professionalizing seminars are planned. Learning assessment procedures
- The method of carrying out the evaluation test is ORAL. As a result of the new provisions and educational needs arising from the health emergency, the examinations are carried out in telematic mode on Google Meet platform until new provisions.
The student can choose mode 1 or 2 for the conduct of the exam.
MODE 1 WITH PROJECT WORK The candidate is asked to develop in advance a structured project work at least 11 pharmaceutical molecules 1 for each of the 11 therapeutic categories carried out in class. It must be sent in ppt format, to the teacher at least 3 days before the starting date of the appeal.
MODE 2 WITHOUT PROJECT WORK At least 10 open questions will be submitted to the candidate.
In both modes the candidate for each of the structure formulas reported and shared on screen is required to describe the structure of the pharmacophore and for the most significant active ingredients in the class, know the structural modulations that the pharmacophore has undergone and with what purposes.
Understand for each class of drugs the relationship between the chemical structure and the activity of the drug. Understand the mechanism of action and therefore the pathophysiological processes with which the drug interferes.
Know how to apply the knowledge of organic chemistry to the discussion of chemical structures of active ingredients and to the commentary of the models of chemical interaction with biological macromolecules; know how to justify on the basis of the chemical structure the pharmacodynamic and pharmacokinetic profile of active ingredients. The student must demonstrate the ability to cross-link the topics addressed in the program.
The student will be assessed for his ability to communicate with clarity and good command of language even rather complex concepts of organic chemistry; analyze the elements that make up a chemical structure to deduce its belonging to a class, to attribute to the molecule as a whole a mechanism, a property or the ability to interact chemically with biological targets; develop the ability to think critically about problems in the chemical-pharmaceutical field and the candidate will be asked for each of the structure formulas reported and shared on screen to describe the structure of the pharmacophore and for the most significant active ingredients of the class, indicated by the teacher, to know the structural modulations that the pharmacophore has undergone and with what purposes. Reference texts
- Alberto Gasco,Fulvio Gualtieri, Carlo Melchiorre - Chimica farmaceutica - Casa Editrice Ambrosiana 2019.
W. O. Foye - Principi di Chimica Farmaceutica - Piccin, Padova 2021
G. L. Patrick. Chimica Farmaceutica. Edises Ed. III/2015
Giovanni Greco. Farmacocinetica e farmacodinamica su basi chimico-fisiche. ISBN Napoli, 2009
