179250-28-3Relevant academic research and scientific papers
(2-benzylphenyl)piperazine derivatives and use thereof
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Paragraph 0142; 0148; 0149; 0150; 0151, (2019/11/19)
The invention discloses (2-benzylphenyl)piperazine derivatives, a use thereof, and a medicinal composition comprising above compounds. The derivatives and the medicinal composition are used for inhibiting serotonin reuptake. The invention also relates to
1-(2-PHENOXYMETHYLPHENYL)PIPERAZINE COMPOUNDS
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Page/Page column 15, (2011/08/03)
The invention relates to compounds of formula I: where a, and R1 through R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhi
Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands
Marinkovic, Dragan,Tucci, Fabio C.,Tran, Joe A.,Fleck, Beth A.,Wen, Jenny,Chen, Chen
scheme or table, p. 4817 - 4822 (2009/05/26)
A series of piperazinebenzylalcohols were prepared and studied to compare with their ketone and amine analogs as MC4R antagonists. Several benzylalcohols such as 14a and 14g displayed low nanomolar binding affinities (Ki 10 nM), and high sele
Synthesis and Structure-Activity Relationships of Novel Arylpiperazines as Potent and Selective Agonists of the Melanocortin Subtype-4 Receptor
Richardson, Timothy I.,Ornstein, Paul L.,Briner, Karin,Fisher, Matthew J.,Backer, Ryan T.,Biggers, C. Kelly,Clay, Michael P.,Emmerson, Paul J.,Hertel, Larry W.,Hsiung, Hansen M.,Husain, Saba,Kahl, Steven D.,Lee, Jonathan A.,Lindstrom, Terry D.,Martinelli, Michael J.,Mayer, John P.,Mullaney, Jeffery T.,O'Brien, Thomas P.,Pawlak, Joseph M.,Revell, Kevin D.,Shah, Jikesh,Zgombick, John M.,Herr, R. Jason,Melekhov, Alex,Sampson, Peter B.,King, Chi-Hsin R.
, p. 744 - 755 (2007/10/03)
The melanocortin receptors have been implicated as potential targets for a number of important therapeutic indications, including inflammation, sexual dysfunction, and obesity. We identified compound 1, an arylpiperazine attached to the dipeptide H-D-Tic-D-p-Cl-Phe-OH, as a novel melanocortin subtype-4 receptor (MC4R) agonist through iterative directed screening of nonpeptidyl G-protein-coupled receptor biased libraries. Structure-activity relationship (SAR) studies demonstrated that substitutions at the ortho position of the aryl ring improved binding and functional potency. For example, the o-isopropyl-substituted compound 29 (Ki = 720 nM) possessed 9-fold better binding affinity compared to the unsubstituted aryl ring (Ki = 6600 nM). Sulfonamide 39 (Ki = 220 nM) fills this space with a polar substituent, resulting in a further 2-fold improvement in binding affinity. The most potent compounds such as the diethylamine 44 (Ki = 60 nM) contain a basic group at this position. Basic heterocycles such as the imidazole 50 (Ki = 110 nM) were similarly effective. We also demonstrated good oral bioavailability for sulfonamide 39.
Aryl piperazine melanocortin MC4 receptor agonists
Dyck, Brian,Parker, Jessica,Phillips, Teresa,Carter, Lee,Murphy, Brian,Summers, Robin,Hermann, Julia,Baker, Tracy,Cismowski, Mary,Saunders, John,Goodfellow, Val
, p. 3793 - 3796 (2007/10/03)
Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC50=24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds
Substituted aryl piperazines as neurokinin antagonists
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, (2008/06/13)
Disclosed are substituted aryl piperazines of Formula I STR1 are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis. In particular compounds of Formula I are shown to be neurokinin antagonists.
