STRATEGIE PER LA SINTESI DI MOLECOLE BIOLOGICAMENTE ATTIVE

Irene IZZO STRATEGIE PER LA SINTESI DI MOLECOLE BIOLOGICAMENTE ATTIVE

8803300011
DEPARTMENT OF CHEMISTRY AND BIOLOGY "ADOLFO ZAMBELLI"
P.H.D. COURSE
CHEMICAL, BIOLOGICAL AND ENVIRONMENTAL SCIENCES
2022/2023

OBBLIGATORIO
YEAR OF COURSE 3
YEAR OF DIDACTIC SYSTEM 2020
AUTUMN SEMESTER
CFUHOURSACTIVITY
1SINTESI E SVILUPPO DI NUOVI FARMACI: DAL LABORATORIO ALL'IMPIANTO PILOTA
0.54LESSONS
2CARBOIDRATI: DALLA SINTESI ALLE APPLICAZIONI TERAPEUTICHE.
0.54LESSONS
Objectives
PRESENT THE VARIOUS ASPECTS OF MODERN GLYCOCHEMISTRY. EXPLAIN THE BIOLOGICAL AND THERAPEUTIC INTEREST OF SUGARS AND THEIR ANALOGS. DESIGN EFFICIENT STRATEGIES FOR THE SYNTHESIS OF GLYCOMIMETICS OF BIOLOGICAL INTEREST.
FURTHERMORE, THE COURSE INTENDS TO PROVIDE INFORMATION RELATING TO PROBLEMS OF SYNTHESIS, PRODUCTION AND MARKETING OF APIS (ACTIVE PHARMACEUTICAL INGREDIENTS) AND PHARMACEUTICAL INTERMEDIATES, FOCUSING BOTH ON PROCESS ASPECTS, SUCH AS SCALING, AND ON PATENT AND REGULATORY.
Prerequisites
ADVANCED KNOWLEDGE IN ORGANIC CHEMISTRY
Contents
BACKGROUND
CARBOHYDRATE ARE UBIQUITOUS IN NATURE AND PLAY KEY ROLES IN A DIVERSITY OF BIOLOGICAL EVENTS INCLUDING VIRAL INFECTION OR INFLAMMATION. GLYCOMIMETICS AS STRUCTURALLY ALTERED ANALOGUES OF SUGARS OFFER THE OPPORTUNITY TO EMULATE CARBOHYDRATE ACTIVITIES, WHILE CIRCUMVENTING THEIR DRAWBACKS AS CREDIBLE DRUGS. STRUCTURAL MODIFICATIONS ARE PERFORMED NOT ONLY TO ENHANCE TARGET AFFINITY AND SELECTIVITY, BUT ALSO TO IMPROVE DRUG-LIKE PROPERTIES, INCLUDING ORAL BIOAVAILABILITY OR IN VIVO STABILITY. WITH REGARDS TO SYNTHETIC METHODOLOGIES, THE RELATIVE STRUCTURAL COMPLEXITY OF GLYCOMIMETICS—WITH A HIGH DENSITY OF FUNCTIONAL GROUPS AND ASYMMETRIC CENTERS—ALSO PROVIDES A FORMIDABLE TESTING GROUND FOR KNOWN REACTIONS WHILE PERMITTING ACCIDENTAL DISCOVERIES IN SYNTHESIS.

OUTLINE
MONOSACCHARIDES
1. DEFINITIONS; 2. RING CONFORMATIONS; 3. ANOMERIC EFFECT
INTRODUCTION TO GLYCOBIOLOGY
1. STRUCTURAL DIVERSITY; 2. BIOLOGICAL INTEREST OF SUGARS; 3. THERAPEUTIC APPLICATIONS
GLYCOMIMETICS
1. C-GLYCOSIDES. 2. CARBASUGARS. 3. IMINOSUGARS

TRANSFER OF A PROCESS FROM THE LABORATORY TO THE PRODUCTION PLANT; EVALUATION OF SCALE-DEPENDENT PROCESS PARAMETERS; STUDY THE BEHAVIOR OF A REACTION UNDER DESIGNED PROCESS CONDITIONS AND PREDICT POTENTIAL DEVIATIONS. THE CGMP (GOOD MANUFACTURING PRACTICE) CERTIFICATIONS FOR APIS: FROM THE R&D LABORATORY TO PRODUCTION; PRODUCE IN A GMP COMPANY (AUTHORIZATIONS, PLANTS, QUALITY SYSTEM, ETC.); PRODUCE A GMP PRODUCT (VALIDATIONS, BATCH RECORDS, ANALYSES). MULTIDISCIPLINARY APPROACH FOR THE DEVELOPMENT AND APPROVAL OF GENERIC DRUGS OF "COMPLEX DRUGS". PATENT ASPECTS, PROCESS DEVELOPMENT, ANALYTICAL CHARACTERIZATIONS, DEMONSTRATION OF BIOEQUIVALENCE, REGULATORY ASPECTS.
Teaching Methods
THE TEACHING WILL BE 4 HOURS OF CLASSROOM LESSONS AND POWERPOINT PRESENTATION. THERE WILL BE PDF FILES AVAILABLE TO THE ATTENDING STUDENTS.
Verification of learning
DISCUSSION IN CLASS OF RESEARCH PAPER IN THE LITERATURE.
Texts
T. K. LINDHORST, ESSENTIALS OF CARBOHYDRATE CHEMISTRY AND BIOCHEMISTRY; WILEY, 2007
M. E. TAYLOR, K. DRICKAMER, INTRODUCTION TO GLYCOBIOLOGY; OXFORD UNIVERSITY PRESS, 2003
More Information
FURTHER INFORMATION CAN BE REQUESTED BY E-MAIL: IIZZO@UNISA.IT, AMASSA@UNISA.IT

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