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Desarollo de derivados de 4-hidroxicumarina con diferente actividad farmacológica

Serra, Silvia (2012) Desarollo de derivados de 4-hidroxicumarina con diferente actividad farmacológica. [Doctoral Thesis]

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Abstract

This dissertation is an interdisciplinary work focused on the discovery and development of new drugs. It includes organic synthesis methodologies and pharmacological evaluation elements seeking structure-activity relationships that allow us to rationally guide the design of new structures with improved properties. Continuing the work that has been made in our research group, we have first synthesized and studied a series of coumarin-resveratrol analogs incorporating an hydroxyl group at the 4 position of the prototype 3-arylcoumarin. This modification allows us also to approach to other type of compounds, isoflavones, that are very abundant in nature. Subsequently we have prepared and studied a series of other different derivatives where the hydroxyl group at the 4 position has been replaced by a benzyloxy group. The preparation of the desired compounds has been performed by using parallel synthesis strategies; that means efficient and easily reproducible synthetic procedures for the production of a number of products in sufficient quantities for pharmacological evaluation. The preliminary biological essays indicate that some of the studied compounds seems to be active against Staphylococcus Aureus and Tenacibaculum Maritimum bacterial strains. Additionally, some other compounds are inhibitors of MAO-B and they also showed an interesting antioxidant activity. The compounds tested for their cytotoxicity activity against MCF-7 and HL-60 cell lines have shown good results. The series of compounds studied allow us to establish the basic structural requirements to modulate the pharmacological properties, opening up a very interesting research path.

Item Type:Doctoral Thesis
Date:15 March 2012
Tutor:Delogu, Giovanna, Santana Penín, Lourdes, Uriarte Villares, Eugenio
PhD classes:Ciclo 24 > Scienze e tecnologie farmaceutiche
Coordinator:Maccioni, Elias
Institution:Universita' degli Studi di Cagliari
Divisions:Dipartimenti (fino a dicembre 2011) > Dipartimento Farmaco chimico tecnologico
Subjects:Area 03 - Scienze chimiche > CHIM/06 Chimica organica
Uncontrolled Keywords:4-idrossicumarine, IMAO, antitumorali, antibatterici, 4-hydroxycoumarins, IMAO, antitumoral, antibacterial
ID Code:689
Deposited On:19 Mar 2012 11:12

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