| Titre : |
Drug-containing NHC-Gold complexes for biomedical applications |
| Type de document : |
texte imprimé |
| Auteurs : |
Álvarez Álvaro Fernández, Auteur ; Catherine Hemmert, Directeur de thèse ; Heinz Gornitzka, Directeur de thèse |
| Langues : |
Anglais (eng) |
| Tags : |
MALARIA GOLD NHC ARTEMISININ TRICLOSAN |
| Résumé : |
"Malaria is the most important parasitic infection in people, threatening around 40% of the human population. In the last years it has become a bigger public health concern because of the augmentation of malaria parasites resistant to artemisinin and its derivatives. Some NHC-gold(I) complexes show antimalarial activities, being a very promising alternative in malaria treatment because of their potential to inhibit thioredoxin reductase (TrxR) that plays a major role in mitochondrial respiratory chain (one of the two pathways that remains active in the quiescent state of the resistant parasites). In this work of thesis a panel of drug-NHC-gold(I) complexes including artemisinin and triclosan moieties has been synthesized and characterized with the objective of developing hybrid molecules with a dual mode of action able to overcome plasmodium resistance to artemisinin and its derivatives. The first group of molecules concerns a family of aliphatic or aromatic-functionalized cationic bis-NHC-gold(I) and neutral mono-NHC-gold(I) complexes with an artemisinin moiety connected through an aliphatic linker. The group includes three series depending on the length of the aliphatic linker (C3, C4, and C5). The three series have been tested against the sensible F32-TEM strain of P. falciparum showing high activities with IC50 values in the nM range. The second group concerns a series of aliphatic or aromatic-functionalized bis-NHC-gold(I) complexes with an triclosan moiety connected through an aliphatic linker. Triclosan inhibits the fatty acid synthesis pathway, which also remains active in the quiescent state on resistant parasites. These complexes were tested against P. falciparum showing, high activities with IC50 values in the nM range. The ligands of this series and their respective complexes have been also tested against one of the leishmaniosis causing parasites, L. infantum, being very effective in both, amastigote and promastigote forms, with IC50 values in the low µM range." |
| Document : |
Thèse de Doctorat |
| Etablissement_delivrance : |
Université de Toulouse 3 |
| Date_soutenance : |
28/09/2018 |
| Ecole_doctorale : |
Sciences de la matière (SdM) Toulouse |
| Domaine : |
Chimie, Biologie, Santé |
| En ligne : |
http://thesesups.ups-tlse.fr/4056/ |
Drug-containing NHC-Gold complexes for biomedical applications [texte imprimé] / Álvarez Álvaro Fernández, Auteur ; Catherine Hemmert, Directeur de thèse ; Heinz Gornitzka, Directeur de thèse . - [s.d.]. Langues : Anglais ( eng)
| Tags : |
MALARIA GOLD NHC ARTEMISININ TRICLOSAN |
| Résumé : |
"Malaria is the most important parasitic infection in people, threatening around 40% of the human population. In the last years it has become a bigger public health concern because of the augmentation of malaria parasites resistant to artemisinin and its derivatives. Some NHC-gold(I) complexes show antimalarial activities, being a very promising alternative in malaria treatment because of their potential to inhibit thioredoxin reductase (TrxR) that plays a major role in mitochondrial respiratory chain (one of the two pathways that remains active in the quiescent state of the resistant parasites). In this work of thesis a panel of drug-NHC-gold(I) complexes including artemisinin and triclosan moieties has been synthesized and characterized with the objective of developing hybrid molecules with a dual mode of action able to overcome plasmodium resistance to artemisinin and its derivatives. The first group of molecules concerns a family of aliphatic or aromatic-functionalized cationic bis-NHC-gold(I) and neutral mono-NHC-gold(I) complexes with an artemisinin moiety connected through an aliphatic linker. The group includes three series depending on the length of the aliphatic linker (C3, C4, and C5). The three series have been tested against the sensible F32-TEM strain of P. falciparum showing high activities with IC50 values in the nM range. The second group concerns a series of aliphatic or aromatic-functionalized bis-NHC-gold(I) complexes with an triclosan moiety connected through an aliphatic linker. Triclosan inhibits the fatty acid synthesis pathway, which also remains active in the quiescent state on resistant parasites. These complexes were tested against P. falciparum showing, high activities with IC50 values in the nM range. The ligands of this series and their respective complexes have been also tested against one of the leishmaniosis causing parasites, L. infantum, being very effective in both, amastigote and promastigote forms, with IC50 values in the low µM range." |
| Document : |
Thèse de Doctorat |
| Etablissement_delivrance : |
Université de Toulouse 3 |
| Date_soutenance : |
28/09/2018 |
| Ecole_doctorale : |
Sciences de la matière (SdM) Toulouse |
| Domaine : |
Chimie, Biologie, Santé |
| En ligne : |
http://thesesups.ups-tlse.fr/4056/ |
|  |
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