52536-36-4Relevant academic research and scientific papers
Synthesis of new 1,2,3-benzotriazin-4-one-arylpiperazine derivatives as 5-HT(1A) serotonin receptor ligands
Caliendo, Giuseppe,Fiorino, Ferdinando,Grieco, Paolo,Perissutti, Elisa,Santagada, Vincenzo,Severino, Beatrice,Bruni, Giancarlo,Romeo, Maria Rosaria
, p. 533 - 538 (2007/10/03)
A series of novel 1,2,3-benzotriazin-4-one derivatives was prepared and evaluated as ligands for 5-HT receptors. Radioligand binding assays proved that the majority of the novel compounds behaved as good to excellent ligands at the 5-HT(1A) receptor, some of which were selective with respect 5-HT(2A) and 5-HT(2C) receptors. Six analogues (1a, 2a, 2b, 2c, 2e and 2i) were selected and further evaluated for their binding affinities on D1, D2 dopaminergic and α1-, α2-adrenergic receptors. A o-OCH3 derivative (2e) bound at 5-HT(1A) sites with subnanomolar affinity (IC50=0.059 nM) and shows high selectivity over all considered receptors and may offer a new lead for the development of therapeutically efficacious agents. Copyright (C) 2000 Elsevier Science Ltd.
Synthesis and trazodone-like pharmacological profile of 1- and 2--propyl>benzotriazoles
Caliendo, G.,Carlo, R. Di,Meli, R.,Perissutti, E.,Santagada, V.,et al.
, p. 969 - 974 (2007/10/02)
A series of 1- and 2--propyl>benzotriazoles were prepared and evaluated for their trazodone-like pharmacological profile; as preliminary pharmacological screening, the compounds were tested for their antiserotonergic, antiadrenergic and antihistaminic in vitro activity as well as for their analgesic in vivo action.Structure-activity relationships showed that among the synthesized compounds, the analogues bearing on the 4-piperazine nitrogen either an unsubstituted phenyl ring or a 2- or 3-chloro phenyl moiety show a pharmacological profilesimilar to that of the antidepressant trazodone. benzotriazoles / antiserotonergic / antiadrenergic / antihistaminic/ analgesic
Synthesis and Biological Activities of 3-Substituted 1-Aryloxyaminopropanes
Agarwal, Shiv K.,Kumar, Yatendra,Saxena, Anil K.,Jain, Padam C.,Anand, Nitya
, p. 435 - 439 (2007/10/02)
A number of 3-substituted 1-aryloxyaminopropanes (9-43) have been prepared by the reaction of appropriate hydroxyaryl compound with 1-chloro-3-1-(N4-aryl-piperazinyl/piperidinyl)>propanes (1-8).The 1-(6/7-quinolyloxy)-3-substituted
