502649-25-4Relevant articles and documents
Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists
Budde, Thomas,Grey, Lucie,Heitman, Laura H.,Hundehege, Petra,Isaak, Andreas,Junker, Anna,Koch, Oliver,Michetti, Lucia,Patberg, Marius,Schulte, Janine,Vinnenberg, Laura,van der Horst, Cas,Füsser, Friederike,Ortiz Zacarías, Natalia V.
, (2021/09/28)
The P2X7 receptor (P2X7R) stands out among the purinergic receptors due to its strong involvement in the regulation of tumor growth and metastasis formation as well as in innate immune responses and afferent signal transmission. Numerous studies have pointed out the beneficial effects of P2X7R antagonism for the treatment of a variety of cancer types, inflammatory diseases, and chronic pain. Herein we describe the development of novel P2X7R antagonists, incorporating piperazine squaric diamides as a central element. Besides improving the antagonists’ potency from pIC50 values of 5.7–7.6, ADME properties (logD7.4 value, plasma protein binding, in vitro metabolic stability) of the generated compounds were investigated and optimized to provide novel P2X7R antagonists with drug-like properties. Furthermore, docking studies revealed the antagonists binding to the allosteric binding pocket in two distinct binding poses, depending on the substitution of the central piperazine moiety.
PIPERAZINE DERIVATIVES AS ANTIVIRAL AGENTS WITH INCREASED THERAPEUTIC ACTIVITY
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Page/Page column 21; 22, (2017/09/15)
The present invention provides 2-phenylpiperazine derivatives having a benzofuran-2-yl group which contributes to increase the antiviral activity as well as, for some substituents, the CC50, giving more active and less cytotoxic compounds. Alth
Piperazine derivatives and the use thereof as medicament
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Paragraph 0302; 0303; 0304; 0305; 0306, (2015/04/21)
The present inventions relate to substituted piperazine derivatives of general formula (I) and to the manufacture of said compounds, pharmaceutical compositions comprising a compound according to general formula (I), and the use of said compounds for the treatment of various medical conditions related to glycine transporter-1 (GlyT1).