2017/2018

2018/2019

DM270

CHIM/08 (PHARMACEUTICAL CHEMISTRY)

DEPARTMENT OF MOLECULAR MEDICINE

MEDICAL AND PHARMACEUTICAL TECHNOLOGIES

Farmaceutico:Biotecnologie farmaceutiche per la ricerca e sviluppo

2°

1st semester (16/10/2018 - 18/01/2019)

9

72 lesson hours

Italian

ORAL TEST

DE LORENZI ERSILIA (titolare) - 3 ECTS
BAVARO TEODORA - 3 ECTS
COLLINA SIMONA - 3 ECTS

BIOSYNTHESIS OF DRUGS - Prof. Teodora Bavaro
To attend this course basic knowledge of biochemistry and enzymology is required

RATIONAL DRUG DESIGN- Prof. SimonaCollina
To attend this course basic knowledge of organic and medicinal chemistry is required

ADVANCED TECHNOLOGIES FOR DRUG ANALYSIS - Prof Ersilia De Lorenzi
To attend this course basic knowledge of HPLC and capillary electrophoresis is required

BIOSYNTHESIS OF DRUGS
This part of the course aim to provide a suitable knowledge on the use of bio-catalysis in the production of drugs, with particular care to the development of engineered bio-catalyst as well as to the regulatory requirement in pharmaceutical industries

RATIONAL DRUG DESIGN
To provide students with the core skills and knowledge on the methodologies used for the rational drug design as well as on the role of Computer Aided Drug Design (CADD) in the drug discovery process.

ADVANCED TECHNOLOGIES FOR DRUG ANALYSIS
The aim of this part of the course is to provide advanced knowledge on Analysis of Biopharmaceuticals, including instrumental aspects, applications and method validation (ICH documents).

BIOSYNTHESIS OF DRUGS
Properties and catalytic mechanism of enzymes (lipase, esterase, penicillin G acylase, nucleoside phosphorylase, nucleoside deoxyribosyltransferase, glycosidase,glycosyltransferase and deoxyribonucleotide kinase), Study of the main enzymatic processes used in the production of drugs (beta-lactam antibiotics oligosaccharides, nucleosides and nucleotides). Application of protein engineering for the development of efficient biocatalysts (immobilization techniques of enzymes). Development of industrial bioprocesses and main regulatory aspect required for the production of Active Pharmaceutical Ingredients.

RATIONAL DRUG DESIGN
Principles of molecular modeling. The process of drug discovery and development: from the identification of novel drug targets to the introduction of new drugs into clinical practice. Lead generation approaches in drug discovery: screening of compound libraries, in silico screening, fragment-based approach, multitarget ligands.
CADD: structure-based and ligand-based drug design. Homology modeling. Molecular docking. Quantitative structure-activity relationship studies (QSAR). Pharmacophore model development. Virtual screening. Rational design of peptide-mimics by means of molecular modeling methods.

ADVANCED TECHNOLOGIES FOR DRUG ANALYSIS
Introduction. Capillary electrophoresis, CE (Modes: MEKC, CCE, CEC, CGE, CIEF, CITP).. Affinity Capillary electrophoresis (ACE). ICH documents relevant to the analysis of biotechnological drugs (Topic Q6B Specifications: Test procedures and acceptance criteria for biotechnological/biological product; Topic Q1A Stability testing Guidelines. Stability testing of new drug substances and products; Topic Q5C Quality of Biotechnological Products: Stability testing of biotechnological/biological products). Reading and discussion of research papers.

BIOSYNTHESIS OF DRUGS
Teaching methods used in the course include lectures performed using slides

RATIONAL DRUG DESIGN
Teaching methods used in the course include lectures, problem-based learning groups, independent study. Various problem assignments are given to the students during the course to illustrate the course content. Discussion of the lecture topics during class is welcomed.

ADVANCED TECHNOLOGIES FOR DRUG ANALYSIS
Reading and discussion of research papers will be part of the course.

BIOSYNTHESIS OF DRUGS
material will be provided by the professor including suitable references to scientific journals.

RATIONAL DRUG DESIGN
Study texts furnished by the teacher are available on Kiro platform
(website: http://elearning1.unipv.it/).
Foye's Principles of Medicinal Chemistry Hardcover – March 8, 2012 by David
A. Williams PhD (Editor)
Wilson and Gisvold's Textbook of Organic Medicinal and Pharmaceutical
Chemistry Hardcover – March 2, 2010 by John M. Beale Jr. PhD (Editor), John
Block (Editor).

ADVANCED TECHNOLOGIES FOR DRUG ANALYSIS
ICH documents.
Handouts

Oral exam. The student is requested to be able to integrate the contents of the three modules (biosynthesis, design and analysis of biotechnologycal drugs).

Oral exam. The student is requested to be able to integrate the contents of the three modules (biosynthesis, design and analysis of biotechnologycal drugs).