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

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-20617271

RESUMO

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.


Assuntos
Adenosina/síntese química , Agonistas do Receptor Purinérgico P1/síntese química , Antagonistas de Receptores Purinérgicos P1/síntese química , Receptores Purinérgicos P1/metabolismo , Triazóis/química , Adenosina/farmacologia , Animais , Linhagem Celular , AMP Cíclico/biossíntese , Humanos , Estrutura Molecular , Agonistas do Receptor Purinérgico P1/farmacologia , Antagonistas de Receptores Purinérgicos P1/farmacologia
3.
Phys Chem Chem Phys ; 12(22): 5841-5, 2010 Jun 14.
Artigo em Inglês | MEDLINE | ID: mdl-20458376

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-19836950

RESUMO

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.


Assuntos
Antagonistas do Receptor A1 de Adenosina , Adenosina/análogos & derivados , Anilidas/farmacologia , Desenho de Fármacos , Receptores Opioides mu/antagonistas & inibidores , Adenosina/síntese química , Adenosina/química , Adenosina/farmacologia , Anilidas/síntese química , Anilidas/química , Ligantes , Estrutura Molecular , Estereoisomerismo , Relação Estrutura-Atividade
5.
Chem Commun (Camb) ; 52(56): 8753-6, 2016 Jul 05.
Artigo em Inglês | MEDLINE | ID: mdl-27339101

RESUMO

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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