22100-10-3Relevant academic research and scientific papers
Preparation, in vitro screening and molecular modelling of mono-quaternary compounds related to the selective acetylcholinesterase inhibitor BW284c51
Benek, Ondrej,Musilek, Kamil,Horova, Anna,Dohnal, Vlastimil,Dolezal, Rafael,Kuca, Kamil
, p. 21 - 29 (2015/04/14)
This paper describes preparation and in vitro evaluation of 19 compounds related to the selective experimental cholinesterase inhibitor BW284c51. The novel compounds were prepared as fragments of parent molecule BW284c51 and evaluated on the model of human recombinant acetylcholinesterase and human plasmatic butyrylcholinesterase. The IC50 values of the prepared compounds were compared to the parent molecule BW284c51. None of the compounds was superior to the parent drug, but two BW284c51 fragments showed promising hAChE inhibition in μM scale and improved selectivity. These two fragments were further subjected to the molecular modelling study and their enzyme interactions were rationalized. The structure-activity relationship of the prepared series was stated.
Dynamic Covalent Chemistry of Nucleophilic Substitution Component Exchange of Quaternary Ammonium Salts
Kulchat, Sirinan,Lehn, Jean-Marie
, p. 2484 - 2496 (2015/11/02)
Dynamic covalent libraries (DCLs) of quaternary ammonium cations were set up by reversible nucleophilic substitution (SN2′ and SN2) exchange reactions of ammonium salts and tertiary amines. The reactions were conducted at 60 °C to generate thermodynamically and kinetically controlled mixtures of quaternary ammonium compounds and tertiary amines, and were accelerated by using iodide as a nucleophilic catalyst. Microwave irradiation was used to assist the exchange reaction between the pyridinium salts and pyridine derivatives. Finally, experiments towards the generation of dynamic ionic liquids were performed. The results of this study pave the way for the extension of dynamic combinatorial chemistry to nucleophilic substitution reactions.
INTRAMOLECULAR THERMAL CYCLIZATION OF QUARTERNARY AMMONIUM SALTS WITH THE PARTICIPATION OF THE AROMATIC RING OF AN ARYLMETHYL GROUP AS A DIENE FRAGMENT
Babayan, A. T.,Torosyan, G. O.,Gekchyan, G. G.,Mkrtchyan, R. S.,Tagmazyan, K. Ts.,Mushegyan, A. V.
, p. 380 - 383 (2007/10/02)
The intramolecular thermal cyclization dimethylallylbenzylammonium bromide and dimethylallyl (α-methylnaphtyl)ammonium chloride led to the formation of 2,2-dimethyl-7,7a-dihydro-vinyleneisoindolinium bromide and 2,2-dimethyl-7,7a-dihydro-3a,6-vinyleneisoi
