51299-21-9Relevant academic research and scientific papers
Novel aryl piperazines for alleviation of ‘andropause’ associated prostatic disorders and depression
Gupta, Sonal,Pandey, Deepti,Mandalapu, Dhanaraju,Sharma, Vikas,Shukla, Mahendra,Singh, Seema,Singh, Nidhi,Yadav, Santosh Kumar,Tanpula, Dilip Kumar,Singh, Surabhi,Maikhuri, Jagdamba P.,Shukla, Shubha,Lal, Jawahar,Siddiqi, Mohammad I.,Gupta, Gopal,Sharma, Vishnu L.
, p. 204 - 218 (2017)
A series of seventeen piperazine derivatives have been synthesized and biologically evaluated for the management of andropause-associated prostatic disorders and depression. Five compounds 16, 19, 20, 21 and 22 significantly inhibited proliferation of and
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.
