92043-13-5Relevant academic research and scientific papers
N-(4-[18F]-fluoropyridin-2-yl)-N-{2-[4-(2-methoxyphenyl) piperazin-1-yl]ethyl}carboxamides as analogs of WAY100635. New PET tracers of serotonin 5-HT1A receptors
García, Gonzalo,Abet, Valentina,Alajarín, Ramón,álvarez-Builla, Julio,Delgado, Mercedes,García-García, Luis,Bascu?ana-Almarcha, Pablo,Pe?a-Salcedo, Carmen,Kelly, James,Pozo, Miguel A.
supporting information, p. 795 - 806 (2014/09/29)
N-(4-[18F]-Fluoropyridin-2-yl)-N-{2-[4-(2-methoxyphenyl) piperazin-1-yl]ethyl}-carboxamides were prepared by labeling their 4-nitropyridin-2-yl precursors through nitro substitution by the 18F anion. In vitro and in vivo tests showed
Synthesis and pharmacological evaluation of [(4-Arylpiperazin-1-yl)-alkyl]- carbamic acid ethyl ester derivatives as potential anxiolytic agents
Khatri, Manisha,Rai, Santosh K.,Ranbhor, Ranjit,Kishore, Krishna,Tiwari, Manisha
experimental part, p. 1143 - 1152 (2012/11/07)
On the basis of our earlier studies, a series of N-{4-[4-(aryl) piperazin-1-yl]-phenyl}-amine derivatives containing terminal carbamoyl fragment with alkyl spacer of different lengths (15-20) were synthesized as ligands, for 5-hydroxytryptamine-1A (5-HT1A
Synthesis, characterization and in vitro biological studies of novel cyano derivatives of N-alkyl and N-aryl piperazine
Chaudhary, Preeti,Nimesh, Surendra,Yadav, Veena,Verma, Akhilesh Kr.,Kumar, Rupesh
, p. 471 - 476 (2008/02/07)
Cyano derivatives of N-alkyl and N-aryl piperazine have been synthesized and screened for antibacterial and antifungal activities. All the synthesized compounds showed the antibacterial activity against pathogenic strains of Staphylococcus aureus (MTCCB 737), Pseudomonas aeruginosa (MTCCB 741), Streptomyces epidermidis (MTCCB 1824) and Escherichia coli (MTCCB 1652) and antifungal activity against pathogenic strains of Aspergillus fumigatus (ITCC 4517), Aspergillus flavus (ITCC 5192) and Aspergillus niger (ITCC 5405). All compounds showed mild to moderate antimicrobial activity. However, compounds 3c, 4a and 6 showed potent antibacterial activity against pathogenic strains used in the study. Compounds 3a, 3b, 4b, and 4d showed mild to moderate antifungal activity against Aspergillus pathogenic strains. The compounds reported in this study were assessed for there cytotoxicity using MTT colorimetric assay on Hela cells. All the compounds showed cell viability more than the control drug gentamicin, with compound 2 having highest i.e. 95% cell viability.
Novel 5-HT7 receptor inverse agonists. Synthesis and molecular modeling of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides.
Vermeulen, Erik S,van Smeden, Marjan,Schmidt, Anne W,Sprouse, Jeffrey S,Wikstroem, Hakan V,Grol, Cor J
, p. 5451 - 5466 (2007/10/03)
A series of arylpiperazine- and 1,2,3,4-tetrahydroisoquinoline-based arylsulfonamides was synthesized and evaluated for their interactions with the constitutively active 5-HT7 receptor. Effects on basal adenylate cyclase activity were measured using HEK-293 cells expressing the rat 5-HT7. All ligands produced a decrease of adenylate cyclase activity, indicative of their inverse agonism. Additionally, computational studies with a set of 22 inverse agonists, including these novel inverse agonists and inverse agonists known from literature, resulted in a pharmacophore model and a CoMFA model (R2 = 0.97, SE = 0.18). Docking of inverse agonists at the binding site of a model of the helical parts of the 5-HT7 receptor, based on the alpha carbon template for 7-TM GPCRs, revealed interesting molecular interactions and a possible explanation for observed structure-activity relationships.
Phenylpiperazinylalkylamino substituted pyridazinones as potent α1 adrenoceptor antagonists
Barlocco,Cignarella,Dal Piaz,Giovannoni,De Benedetti,Fanelli,Montesano,Poggesi,Leonardi
, p. 2403 - 2410 (2007/10/03)
QSAR models have been used for designing a series of compounds characterized by a N-phenylpiperazinylalkylamino moiety linked to substituted pyridazinones, which have been synthesized. Measurements of the binding affinities of the new compounds toward the
4-Bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2- naphthalenecarboxamides: Selective dopamine D3 receptor partial agonists
Glase, Shelly A.,Akunne, Hyacinth C.,Heffner, Thomas G.,Johnson, Stephen J.,Kesten, Suzanne R.,Mackenzie, Robert G.,Manley, Peter J.,Pugsley, Thomas A.,Wright, Jon L.,Wise, Lawrence D.
, p. 1361 - 1366 (2007/10/03)
A series of 4-bromo-1-methoxy-N-[2-(4-aryl-1-piperazinyl)ethyl]-2- naphthalenecarboxamide dopamine (DA) D3 receptor agonists has been identified. These compounds were found to be selective for DA D3 over D2 receptors and were shown to be partial to full agonists as measured by stimulation of mitogenesis in D3-transfected CHO p-5 cells.
5-HT(1A), and D-2 receptor affinity of o-methoxyphenylpiperazine derivatives with terminal benzamide fragment on N-4 alkyl chain. 2
Perrone,Berardi,Leopoldo,Tortorella,Lograno,Daniele,Govoni
, p. 505 - 510 (2007/10/02)
The synthesis of some o-methoxyphenylpiperazines with a benzamide moiety on N-4 alkyl chain was accomplished and their affinity for dopamine and serotonin receptor subtypes was assayed by in vitro receptor binding. The results show that several derivative
