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1.
Angew Chem Int Ed Engl ; 54(38): 11117-21, 2015 Sep 14.
Artículo en Inglés | MEDLINE | ID: mdl-26234749

RESUMEN

We designed efficient precursors that combine complementary associative groups with exceptional binding affinities and thiocarbonylthio moieties enabling precise RAFT polymerization. Well defined PS and PMMA supramolecular polymers with molecular weights up to 30 kg mol(-1) are synthesized and shown to form highly stable supramolecular diblock copolymers (BCPs) when mixed, in non-polar solvents or in the bulk. Hierarchical self-assembly of such supramolecular BCPs by thermal annealing affords morphologies with excellent lateral order, comparable to features expected from covalent diblock copolymer analogues. Simple washing of the resulting materials with protic solvents disrupts the supramolecular association and selectively dissolves one polymer, affording a straightforward process for preparing well-ordered nanoporous materials without resorting to crosslinking or invasive chemical degradations.

2.
Org Biomol Chem ; 8(17): 3874-81, 2010 Sep 07.
Artículo en Inglés | MEDLINE | ID: mdl-20617271

RESUMEN

The synthesis of new C-6 1,2,3-triazole adenosine derivatives via microwave assisted 1,3-dipolar cycloaddition as key step is described. The binding on membranes of cells that over express A(1) adenosine receptors (A(1)AR) was also evaluated. Among them, four compounds increased cAMP production, in a dose-dependent manner acting as antagonists of the A(1)AR, while two compounds act as agonists.


Asunto(s)
Adenosina/síntesis química , Agonistas del Receptor Purinérgico P1/síntesis química , Antagonistas de Receptores Purinérgicos P1/síntesis química , Receptores Purinérgicos P1/metabolismo , Triazoles/química , Adenosina/farmacología , Animales , Línea Celular , AMP Cíclico/biosíntesis , Humanos , Estructura Molecular , Agonistas del Receptor Purinérgico P1/farmacología , Antagonistas de Receptores Purinérgicos P1/farmacología
3.
Phys Chem Chem Phys ; 12(22): 5841-5, 2010 Jun 14.
Artículo en Inglés | MEDLINE | ID: mdl-20458376

RESUMEN

We have investigated the properties of a series of dinitroxides as polarizing agents for SS NMR/DNP applications. Our results clearly establish that an orthogonal relative orientation of electron g tensors is a crucial requirement to obtain high enhancement DNP factors. Moreover, the ratio of the proton Larmor frequency over the e(-)-e(-) dipolar coupling (omega(H)/omega(D)) influences the efficiency of the cross effect (CE) mechanism, thus the Ree distance between the unpaired electrons must be adapted to omega(H).

4.
Bioorg Med Chem Lett ; 19(23): 6736-9, 2009 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-19836950

RESUMEN

The cross talk between different membrane receptors is the source of increasing research. We designed and synthesized a new hetero-bivalent ligand that has antagonist properties on both A(1) adenosine and mu opiate receptors with a K(i) of 0.8+/-0.05 and 0.7+/-0.03 microM, respectively. This hybrid molecule increases cAMP production in cells that over express the mu receptor as well as those over expressing the A(1) adenosine receptor and reverses the antalgic effects of mu and A(1) adenosine receptor agonists in animals.


Asunto(s)
Antagonistas del Receptor de Adenosina A1 , Adenosina/análogos & derivados , Anilidas/farmacología , Diseño de Fármacos , Receptores Opioides mu/antagonistas & inhibidores , Adenosina/síntesis química , Adenosina/química , Adenosina/farmacología , Anilidas/síntesis química , Anilidas/química , Ligandos , Estructura Molecular , Estereoisomerismo , Relación Estructura-Actividad
5.
Chem Commun (Camb) ; 52(56): 8753-6, 2016 Jul 05.
Artículo en Inglés | MEDLINE | ID: mdl-27339101

RESUMEN

We introduce recodable surfaces solely based on reversible artificial hydrogen bonding interactions. We show that a symmetrical oligoamide (SOA) attached to poly(methyl methacrylate) (PMMA) can be repeatedly immobilized and cleaved off spatially defined surface domains photochemically functionalized with asymmetric oligoamides (AOAs). The spatially resolved recodability is imaged and quantified via ToF-SIMS.

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