116436-03-4Relevant articles and documents
Improved imide receptors by imprinting using pyrimidine-based fluorescent reporter monomers
Manesiotis, Panagiotis,Hall, Andrew J.,Sellergren, Boerje
, p. 2729 - 2738 (2005)
(Chemical Equation Presented) Optically responsive receptors toward imides based on 6-substituted 2,4-bis(acrylamido)pyrimidines are presented. The monomers were readily prepared in good yield. Solution binding to 1-benzyluracil (BU) monitored by 1H NMR appeared lower than a previously reported pyridine-based monomer. However, as indicated by 1H NMR and IR spectral investigations, the association strength was demonstrated to be "masked" by dimerization of the pyrimidine-based monomer units. Thus, from dilution experiments, a dimerization constant of 731 M-1 was estimated for the pyrimidine-based monomer 2,4-bis(acrylamido)-6- piperidinopyrimidine whereas for the pyridine-based monomer 2,6-bis(acrylamido) pyridine, no self-association was observed. This precluded an accurate determination of the binding constant for BU to the former monomer whereas for the latter a binding constant of 757 M-1 was measured. Despite the strong self-association, the novel monomer was shown to lead to enhanced imprinting effects when compared to imprinted polymers prepared analogously, but using the pyridine-based monomer as the recognition element. This was attributed to a higher intrinsic binding affinity exhibited by the pyrimidine based host monomer vis a vis the guest and the existence in the former of more than one interaction site for the guest. The monomers exhibited fluorescence emission informative of the mode of monomer incorporation in the polymer and the presence of guest species. Thus, the fluorescence was rapidly and selectively quenched upon template addition, with the degree of quenching correlating with binding affinity and the amount of template bound to the polymer.
Synthesis of novel 5-amino-thiazolo[4,5-d]pyrimidines as E. coli and S. aureus SecA inhibitors
Jang, Mi-Yeon,Jonghe, Steven De,Segers, Kenneth,Anné, Jozef,Herdewijn, Piet
experimental part, p. 702 - 714 (2011/02/28)
An efficient synthesis of a library of 5-amino-thiazolo[4,5-d]pyrimidines is reported. Regioselective displacements of chlorines, as well as regioselective diazotation reactions are described, which allow the introduction of structural diversity on the sc
5-ARYL-SUBSTITUTED DIHYDROPYRIDOPYRIMIDINES AND DIHYDROPYRIDAZINES AND USE THEREOF AS MINERAL CORTICOID ANTAGONISTS
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Page/Page column 20, (2010/03/02)
The present application relates to novel aryl-substituted heterobicyclic compounds, a process for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prop
