55666-43-8Relevant articles and documents
Fine-tuning water exchange on GdIII poly(amino carboxylates) by modulation of steric crowding
Jaszberenyi, Zoltan,Sour, Angelique,Toth, Eva,Benmelouka, Meriem,Merbach, Andre E.
, p. 2713 - 2719 (2005)
In the objective of optimizing water exchange rate on stable, nine-coordinate, monohydrated GdIII poly(amino carboxylate) complexes, we have prepared monopropionate derivatives of DOTA4- (DO3A-Nprop4-) and DTPA5- (DTTA-Nprop5-). A novel ligand, EPTPA-BAA3-, the bisamylamide derivative of ethylenepropylenetriaminepentaacetate (EPTPA5-) was also synthesized. A variable temperature 17O NMR study has been performed on their GdIII complexes, which, for [Gd(DTTA-Nprop)(H2O)] 2- and [Gd(EPTPA-BAA)(H2O)] has been combined with multiple field EPR and NMRD measurements. The water exchange rates, k ex298, are 8.0 × 107 s-1, 6.1 × 107 s-1 and 5.7 × 107 s -1 for [Gd(DTTA-Nprop)(H2O)]2-, [Gd(DO3A-Nprop)(H2O)]- and [Gd(EPTPA-BAA)(H 2O)], respectively, all in the narrow optimal range to attain maximum proton relaxivities, provided the other parameters (electronic relaxation and rotation) are also optimized. The substitution of an acetate with a propionate arm in DTPA5- or DOTA4- induces increased steric compression around the water binding site and thus leads to an accelerated water exchange on the GdIII complex. The kex values on the propionate complexes are, however, lower than those obtained for [Gd(EPTPA)(H2O)]2- and [Gd(TRITA)(H2O)] - which contain one additional CH2 unit in the amine backbone as compared to the parent [Gd(DTPA)(H2O)]2- and [Gd(DOTA)(H2O)]-. In addition to their optimal water exchange rate, [Gd(DTTA-Nprop)(H2O)]2- has, and [Gd(DO3A-Nprop)(H2O)]- is expected to have sufficient thermodynamic stability. These properties together make them prime candidates for the development of high relaxivity, macromolecular MRI contrast agents. The Royal Society of Chemistry 2005.
Thrombin inhibitors
-
Page column 29, (2010/02/06)
Novel five-membered heterocyclic amidines, their preparation and use as competitive inhibitors of trypsin-like serine proteases, especially thrombin and kininogenases such as kallikrein. Pharmaceutical compositions which contain the compounds as active ingredients, and use of the compounds as thrombin inhibitors, anticoagulants and antiinflammatory agents.
Sulfonyl isatin compounds and methods of blocking apoptosis therewith
-
, (2008/06/13)
-