164934-23-0Relevant academic research and scientific papers
Design, synthesis, and anticonvulsant activity of some derivatives of xanthone with aminoalkanol moieties
Waszkielewicz, Anna M.,S?oczyńska, Karolina,P?kala, El?bieta,?mudzki, Pawe?,Siwek, Agata,Grybo?, Anna,Marona, Henryk
, p. 339 - 352 (2017)
A series of new xanthone derivatives have been synthesized and evaluated for their anticonvulsant properties in the maximal electroshock, subcutaneous metrazole tests and for neurotoxicity in the rotarod in mice, i.p. and rats, p.o. Compound 9: R,S-2-{2-[(1-hydroxybutan-2-yl]amino)ethoxy}-9H-xanthen-9-one and compound 12: R,S-2-{3-[(1-hydroxybutan-2-yl)amino]propoxy}-9H-xanthen-9-one exerted activity in rats, p.o. 2 and 4?h after administration, respectively. Therefore, metabolic stability of the compounds was evaluated with use of rat microsomes, resulting in half-life t1/2 136 and 108?min, respectively, indicating that either the metabolites are very active or the parent compounds exert ADME properties other than metabolism which influence the late onset of activity.
Cholinergic Agents. Synthesis and Acetylcholinesterase Inhibitory Activity of Some ω-[N-Methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyxanthen-9-ones
Valentini, Piero,Rampa, Angela,Bisi, Alessandra,Fabbri, Giuseppina,Andrisano, Vincenza,Cavrini, Vanni
, p. 255 - 264 (2007/10/03)
A series of ω-[N-methyl-N-(3-alkylcarbamoyloxyphenyl)methyl]aminoalkoxyxanthen-9-ones was prepared. The alkoxy chain occupies, alternatively, the positions 2, 3 and 4 of the xanthone moiety and has a variable length. The compounds were evaluated for acetylcholinesterase inhibitory activity. Some in this series were revealed to be more potent than physostigmine. Optimum activity was found with the 3 position and with a four or three carbon chain length separating the benzylamino group from the xanthenonyloxy moiety.
