Masullo, Dario
(2017)
Identification of new synthetic and semi-synthetic derivatives for
the treatment of entero-hepatic disorders.
[Tesi di dottorato]
| Tipologia del documento: |
Tesi di dottorato
|
| Lingua: |
English |
| Titolo: |
Identification of new synthetic and semi-synthetic derivatives for
the treatment of entero-hepatic disorders |
| Autori: |
| Autore | Email |
|---|
| Masullo, Dario | dario.masullo@unina.it |
|
| Data: |
9 Aprile 2017 |
| Numero di pagine: |
200 |
| Istituzione: |
Università degli Studi di Napoli Federico II |
| Dipartimento: |
Farmacia |
| Dottorato: |
Scienza del farmaco |
| Ciclo di dottorato: |
29 |
| Coordinatore del Corso di dottorato: |
| nome | email |
|---|
| D'Auria, Maria Valeria | madauria@unina.it |
|
| Tutor: |
| nome | email |
|---|
| Zampella, Angela | [non definito] |
|
| Data: |
9 Aprile 2017 |
| Numero di pagine: |
200 |
| Parole chiave: |
organic synthesis, medicinal chemistry, bile acids, nuclear receptors, GPCR |
| Settori scientifico-disciplinari del MIUR: |
Area 03 - Scienze chimiche > CHIM/06 - Chimica organica |
[error in script]
[error in script]
| Depositato il: |
26 Apr 2017 21:25 |
| Ultima modifica: |
13 Mar 2018 12:07 |
| URI: |
http://www.fedoa.unina.it/id/eprint/11671 |
| DOI: |
10.6093/UNINA/FEDOA/11671 |
Abstract
Bile acids, the end product of cholesterol metabolism, got researchers attention in
the last twenty years for their ability to act as signal molecules. They are involved
in multiple metabolic processes and, for this reason, they could be interesting lead
compounds for the treatment of various diseases linked to metabolic syndrome.
Due to their small chemical structure, bile acids are promiscuous molecules;
indeed, they are able to bind both nuclear and G-protein coupled receptors, but, in
some cases, in an unspecific manner. This promiscuity could lead to an unwanted
activation of one of the two mentioned receptor class that could results in
undesired side effects. For this reason, it became fundamental to understand the
key pharmacophoric portions in that kind of molecules in order to know which
part of them is responsible for the activation of one or both that receptors class.
In this context, most of my Ph.D. was spent on the speculation on different bile
acid scaffolds, where modifications were done in order understand the selectivity
criteria behind the activation of one of the two receptors classes, improving their
activity towards them. The modifications carried out generated a first class of
novel selective and dual FXR, GPBAR1 (a G-protein coupled receptor) and
LXR
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