347186-48-5Relevant academic research and scientific papers
PIPERAZINE DERIVATIVES FOR INFLUENZA VIRUS INHIBITION
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Page/Page column 27, (2018/08/26)
The present invention provides piperazine derivatives exhibiting high affinity to the stem region (viral membrane proximal part) of influenza hemagglutinin as determined through competition binding and high virus neutralization activity while having low c
INHIBITORS OF (ALPHA-V)(BETA-6) INTEGRIN
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Page/Page column 0271; 0272, (2018/09/16)
Disclosed are small molecule inhibitors of αvβ6 integrin, and methods of using them to treat a number of diseases and conditions.
Discovery and hit-to-lead evaluation of piperazine amides as selective, state-dependent NaV1.7 inhibitors
Sparling, Brian A.,Yi,Able,Bregman,DiMauro, Erin F.,Foti,Gao,Guzman-Perez,Huang,Jarosh,Kornecook,Ligutti,Milgram,Moyer,Youngblood,Yu,Weiss
supporting information, p. 744 - 754 (2017/04/27)
NaV1.7 is a particularly compelling target for the treatment of pain. Herein, we report the discovery and evaluation of a series of piperazine amides that exhibit state-dependent inhibition of NaV1.7. After demonstrating significant pharmacodynamic activity with early lead compound 14 in a NaV1.7-dependent behavioural mouse model, we systematically established SAR trends throughout each sector of the scaffold. The information gleaned from this modular analysis was then applied additively to quickly access analogues that encompass an optimal balance of properties, including NaV1.7 potency, selectivity over NaV1.5, aqueous solubility, and microsomal stability.
Copper-catalyzed amination of silyl ketene acetals with N-chloroamines
Miura, Tomoya,Morimoto, Masao,Murakami, Masahiro
, p. 5214 - 5217,4 (2020/09/02)
A copper(I)/2,2′-bipyridyl complex catalyzes an amination reaction of silyl ketene acetals with N-chloroamines, presenting a new preparative method of α-amino esters.
SUBSTITUTED PIPERAZINES AND PIPERIDINES AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR
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Page/Page column 50, (2010/11/27)
The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.
Privileged structure based ligands for melanocortin receptors - Substituted benzylic piperazine derivatives
Fisher, Matthew J.,Backer, Ryan T.,Collado, Ivan,De Frutos, Oscar,Husain, Saba,Hsiung, Hansen M.,Kuklish, Steve L.,Mateo, Ana I.,Mullaney, Jeffrey T.,Ornstein, Paul L.,Paredes, Cristina Garcia,O'Brian, Thomas P.,Richardson, Timothy I.,Shah, Jikesh,Zgombick, John M.,Briner, Karin
, p. 4973 - 4978 (2007/10/03)
Replacement of the aryl piperazine moiety in compound 1 with a variety of substituted benzylic piperazines (6) yields compounds that afford melanocortin receptor 4 (MCR4) activity. Analogs with ortho substitution on the aromatic ring afforded the highest
Dual NK1 antagonists - Serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives
Ryckmans, Thomas,Berton, Olivier,Grimee, Renee,Kogej, Thierry,Lamberty, Yves,Pasau, Patrick,Talaga, Patrice,Genicot, Christophe
, p. 3195 - 3198 (2007/10/03)
The synthesis, structure-affinity relationship and activity of benzyloxyphenethyl piperazine derivatives combining NK1 antagonism and serotonin reuptake inhibition is described. Compound 7u was shown to be active in animal models of 5-HT reuptake inhibition and central NK1 receptor blockade, and was demonstrated to be orally active in an integrated model sensitive to both mechanisms. This class of compounds potentially represents a new generation of antidepressants.
