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NMR and molecular modelling studies on elastase inhibitor-peptides for wound ma...
Barros, Sandra Cerqueira; Louro, Ricardo O.; Micaelo, N. M.; Martins, José A.; Marcos, João Carlos; Paulo, Artur CavacoProteases play an important and critical role in the physiological process of wound repair. However, excessive and unregulated release of proteolytic enzymes (e.g., elastase) mediates abnormal degradation of healthy tissues, which leads to inflammatory disorders such as chronic wounds. Thus, it is of therapeutic interest to develop novel synthetic inhibitor-peptides of elastase, which can restore the balance be...
Amide conjugates of the DO3A-N-(alfa-amino)propionate ligand : leads for stable...
Ferreira, Miguel Filipe Moreira Marques; Martins, André F.; Martins, Catarina I. O.; Ferreira, Paula M. T.; Tóth, Éva; Rodrigues, Tiago B.A novel synthetic methodology for preparing amide conjugates of the DO3A-N-(alfa-amino)propionate chelator is described, using the synthesis of the DO3A-N-(alfa-benzoylamido)propionate chelator as an illustrative example. The model Gd(DO3A-N-(alfa-benzoylamido)propionate) chelate displays accelerated water exchange, stability in a wide pH range and inertness towards transmetallation by Zn2+. The Gd(DO3A-N-(al...
Synthesis of 2,6-bis-(oxazolyl)pyridine ligands for luminescent Ln(III) complexes
Pereira, Goreti; Ferreira, Paula M. T.; Castanheira, Elisabete M. S.; Martins, José A.; Ferreira, Miguel Filipe Moreira MarquesSubmitted to the European Journal of Organic Chemistry ; New bis-(oxazolyl)pyridine ligands for Ln(III) ions were prepared using a expeditious methodology from threonine and dipicolinic acid chloride. The synthetic strategy includes a dehydration step to give a bis-dehydroaminobutyric acid derivative followed by bromination and cyclization with DBU. Photophysical studies of Eu(III) and Tb(III) complexes of th...
Gold nanoparticles functionalised with stable, fast water exchanging Gd3+ chela...
Ferreira, Miguel Filipe Moreira Marques; Mousavi, Bibimaryam; Ferreira, Paula M. T.; Martins, Catarina; Helm, Lothar; Martins, José A.Gold nanoparticles functionalized with Gd3+ chelates displaying fast water exchange, superb pH stability and inertness towards transmetalation with Zn2+ have been prepared and characterized as a new high relaxivity (29 mM-1s-1, 30 MHz, 25 ºC) Contrast Agent potentially safe for in vivo MRI applications. The Lipari-Szabo treatment for internal rotation was used to evaluate the effect of linker flexibility on the...
Gd(III)-EPTPAC16, a new self-assembling potential liver MRI contrast agent: in ...
Torres, Suzana; Prata, Maria I. M.; Santos, Ana C.; André, João P.; Martins, José A.; Helm, Lothar; Tóth, Éva; García-Martín, Maria L.The recently reported amphiphilic chelate, [Gd(EPTPAC16)(H2O)]2-, forms supramolecular aggregates in aqueous solution by self-assembly of the monomers with a relaxometrically determined critical micellar concentration (CMC) of 0.34 mM. The effect of sonication on the aggregate size was characterized by dynamic light scattering and relaxometry, indicating the presence of premicellar aggregates and an overall dec...
H5EPTPACH2OH: Synthesis, Relaxometric Characterization and 1H NMR Spectroscopic...
Torres, Susana; Martins, José A.; André, João P.; Pereira, Giovannia A.; Kiraly, Robert; Brücher, Ernö; Helm, Lothar; Tóth, ÉvaThe synthesis and characterization of a new metal chelator, 4-(S)-hydroxymethyl-3,6,10-tri(carboxymethyl)-3,6,10-triazadodecanedioic acid (H5EPTPACH2OH), is reported. Protonation constants for the ligand H5EPTPACH2OH and for the previously reported H5EPTPAC16 have been determined by potentiometry, which reveals that both ligands display slightly higher protonation constants relative to that of the ligand DTPA5-...
Supramolecular Assembly of an Amphiphilic GdIII Chelate: Tuning the Reorientati...
Torres, Susana; Martins, José A.; André, João P.; Geraldes, Carlos F. G. C.; Merbach, André E.; Tóth, ÉvaWe report the synthesis and characterization of the novel ligand H5EPTPA-C16 ((hydroxymethylhexadecanoyl ester)ethylenepropylenetriaminepentaacetic acid). This ligand was designed to chelate the GdIII ion in a kinetically and thermodynamically stable way while ensuring an increased water exchange rate (kex) on the GdIII complex owing to steric compression around the water-binding site. The attachment of a palmi...
Lanthanide(III) Chelates of DTPA Bis(amide) Glycoconjugates: Potential Imaging ...
Baía, Paula; André, João P.; Geraldes, Carlos F. G. C.; Martins, José A.; Merbach, André E.; Tóth, ÉvaThe synthesis and characterisation of a new class of DTPA bis(amide) linked glycoconjugates of different sugars [lactose (Lac) and galactose (Gal)] and valencies (di and tetra) and their LnIII complexes is reported. The 1H NMR spectra of the SmIII and EuIII complexes of DTPAGal2, DTPAGal4, and DTPALac2, obtained between 7 and 80 °C, indicate that several of the four possible diastereoisomeric pairs of structure...
Thermodynamic evaluation and modeling of proton and water exchange associated w...
Pereira,M.T.; Silva-Alves,J.M.; Martins-José,A.; Lopes,J.C.D.; Santoro,M.M.Serine-proteases are involved in vital processes in virtually all species. They are important targets for researchers studying the relationships between protein structure and activity, for the rational design of new pharmaceuticals. Trypsin was used as a model to assess a possible differential contribution of hydration water to the binding of two synthetic inhibitors. Thermodynamic parameters for the associatio...
Lanthanide(III) Complexes of DOTA-Glycoconjugates: A Potential New Class of Lec...
André, João P.; Geraldes, Carlos F. G. C.; Martins, José A.; Merbach, André E.; Prata, Maria I. M.; Santos, Ana C.; Lima, João J. P. de; Tóth, ÉvaThe synthesis and characterization of a new class of DOTA (1,4,7,10-tetrakis(carboxymethyl)-1,4,7,10-tetraazacyclododecane) monoamide-linked glycoconjugates (glucose, lactose and galactose) of different valencies (mono, di and tetra) and their SmIII, EuIII and GdIII complexes are reported. The 1H NMR spectrum of EuIII-DOTALac2 shows the predominance of a single structural isomer of square antiprismatic geometry...
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