147197-22-6Relevant academic research and scientific papers
Synthesis and in vitro evaluation of novel non-oximes for the reactivation of nerve agent inhibited human acetylcholinesterase
Horn, Gabriele,Worek, Franz,de Koning, Martijn C.,van Grol, Marco
, (2020/06/04)
Since several decades oximes have been used as part of treatment of nerve agent intoxication with the aim to restore the biological function of the enzyme acetylcholinesterase after its covalent inhibition by organophosphorus compounds such as pesticides and nerve agents. Recent findings have illustrated that, besides oximes, certain Mannich phenols can reactivate the inhibited enzyme very effectively, and may therefore represent an attractive complementary class of reactivators. In this paper we further probe the effect of structural variation on the in vitro efficacy of Mannich phenol based reactivators. Thus, we present the synthesis of 14 compounds that are close variants of the previously reported 4-amino-2-(1-pyrrolidinylmethyl)-phenol, a very effective non-oxime reactivator, and 3 dimeric Mannich phenols. All compounds were assessed for their ability to reactivate human acetylcholinesterase inhibited by the nerve agents VX, tabun, sarin, cyclosarin and paraoxon in vitro. It was confirmed that the potency of the compounds is highly sensitive to small structural changes, leading to diminished reactivation potency in many cases. However, the presence of 4-substituted alkylamine substituents (as exemplified with the 4-benzylamine-variant) was tolerated. More surprisingly, the dimeric compounds demonstrated non-typical behavior and displayed some reactivation potency as well. Both findings may open up new avenues for designing more effective non-oxime reactivators.
Aluminum Complexes of Monopyrrolidine Ligands for the Controlled Ring-Opening Polymerization of Lactide
Beament, James,Mahon, Mary F.,Buchard, Antoine,Jones, Matthew D.
supporting information, p. 1719 - 1724 (2018/06/18)
In this paper we report the full characterization (solution-state NMR spectroscopy and solid-state structures) of a series of Al(III) half-salan complexes and their exploitation for the ring-opening polymerization of rac-lactide. Depending on the ligand e
Potential Antimalarials. XVII. Di- and Mono-Mannich Bases of 2(and 4)-phenol
Barlin, Gordon B.,Nguyen, Trang M. T.,Kotecka, Barbara,Rieckmann, Karl H.
, p. 21 - 29 (2007/10/02)
Di- and mono-Mannich base derivatives of 2(and 4)-phenols have been prepared for comparison with the 7-trifluoromethyl isomers in tests for antimalarial activity.The order of activity in in vitro tests against t
