Masullo, Dario (2017) Identification of new synthetic and semi-synthetic derivatives for the treatment of entero-hepatic disorders. [Tesi di dottorato]

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Item Type: Tesi di dottorato
Lingua: English
Title: Identification of new synthetic and semi-synthetic derivatives for the treatment of entero-hepatic disorders
Creators:
CreatorsEmail
Masullo, Dariodario.masullo@unina.it
Date: 9 April 2017
Number of Pages: 200
Institution: Università degli Studi di Napoli Federico II
Department: Farmacia
Dottorato: Scienza del farmaco
Ciclo di dottorato: 29
Coordinatore del Corso di dottorato:
nomeemail
D'Auria, Maria Valeriamadauria@unina.it
Tutor:
nomeemail
Zampella, AngelaUNSPECIFIED
Date: 9 April 2017
Number of Pages: 200
Uncontrolled Keywords: organic synthesis, medicinal chemistry, bile acids, nuclear receptors, GPCR
Settori scientifico-disciplinari del MIUR: Area 03 - Scienze chimiche > CHIM/06 - Chimica organica
Date Deposited: 26 Apr 2017 21:25
Last Modified: 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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