Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.

Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.

The discovery of (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides and their binding affinities for a selection of 5-HT and dopamine subreceptors is described. Many compounds show high affinity (pK(i)>8) for the 5-HT(6) receptor and >100-fold selectivity against a range of other recepto...

Full description

Bibliographic Details
Main Authors:	Bromidge, S, Griffith, K, Heightman, T, Jennings, A, King, F, Moss, S, Newman, H, Riley, G, Routledge, C, Serafinowska, H, Thomas, DR
Format:	Journal article
Language:	English
Published:	2001

Similar Items

Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry.
by: Corbett, D, et al.
Published: (2005)

1-(Arylsulfonyl-isoindol-2-yl)piperazines as 5-HT<sub>6</sub>R Antagonists: Mechanochemical Synthesis, In Vitro Pharmacological Properties and Glioprotective Activity
by: Vittorio Canale, et al.
Published: (2022-12-01)

Crystal structures of 4-(pyrimidin-2-yl)piperazin-1-ium chloride and 4-(pyrimidin-2-yl)piperazin-1-ium nitrate
by: Thammarse S. Yamuna, et al.
Published: (2014-10-01)

Synthesis and Structure-Activity Relationship Analysis of 5-HT7 Receptor Antagonists: Piperazin-1-yl Substituted Unfused Heterobiaryls
by: Lucjan Strekowski, et al.
Published: (2016-03-01)

The distribution of 5-HT(6) receptors in rat brain: an autoradiographic binding study using the radiolabelled 5-HT(6) receptor antagonist [(125)I]SB-258585.
by: Roberts, J, et al.
Published: (2002)

In Vitro Evaluation of Arylsulfonamide Derivatives against <i>Trypanosoma cruzi</i>
by: Policarpo Ademar Sales Junior, et al.
Published: (2023-06-01)

Design, Synthesis, and Cytotoxic Activity of Novel Natural Arylsulfonamide-Inspired Molecules
by: Wenbo Huang, et al.
Published: (2022-02-01)

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
by: Nuti, E, et al.
Published: (2013)

New Piperazine Derivatives of 6-Acetyl-7-hydroxy-4-methylcoumarin as 5-HT<sub>1A</sub> Receptor Agents
by: Kinga Ostrowska, et al.
Published: (2023-02-01)

Antibacterial Activity of a Promising Antibacterial Agent: 22-(4-(2-(4-Nitrophenyl-piperazin-1-yl)-acetyl)-piperazin-1-yl)-22-deoxypleuromutilin
by: Xiang-Yi Zuo, et al.
Published: (2021-06-01)

Novel Donepezil–Arylsulfonamide Hybrids as Multitarget-Directed Ligands for Potential Treatment of Alzheimer’s Disease
by: Fausto Queda, et al.
Published: (2021-03-01)

Evaluation of the In Vitro Antifungal Activity of Novel Arylsulfonamides against <i>Candida</i> spp.
by: Giovanna Ginestra, et al.
Published: (2023-06-01)

In Silico Design, Synthesis, and Biological Evaluation of Anticancer Arylsulfonamide Endowed with Anti-Telomerase Activity
by: Giulia Culletta, et al.
Published: (2022-01-01)

(1<i>R</i>,2<i>R</i>,6<i>S</i>)-2(4-(4-Isopropylbenzyl)piperazin-1-yl)-3-methyl-6-(prop-1-en-2-yl)cyclohex-3-enol
by: Alexandra V. Podturkina, et al.
Published: (2023-01-01)

Dichlorido(2-{[2-(piperazin-4-ium-1-yl)ethyl] iminomethyl}phenolate)cadmium(II)
by: Salga, M.S., et al.
Published: (2010)

1,4-Bis(2-((1<i>R</i>,5<i>S</i>)-6,6-dimethylbicyclo[3.1.1]hept-2-en-2-yl)ethyl)piperazine
by: Nikolai S. Li-Zhulanov, et al.
Published: (2024-02-01)

Dichlorido(2-{ 2-(piperazin-4-ium-1-yl)ethyl iminomethyl}phenolate)cadmium(II)
by: Salga, M.S., et al.
Published: (2010)

Ultrasonic Synthesis and Preliminary Evaluation of Anticoronaviral Activity of 6,7-Dimethoxy-4-(4-(4-methoxyphenyl)piperazin-1-yl)-1-methylquinolin-1-ium Iodide
by: Aleksey A. Vasilev, et al.
Published: (2022-07-01)

Conformationally Restricted Glycoconjugates Derived from Arylsulfonamides and Coumarins: New Families of Tumour-Associated Carbonic Anhydrase Inhibitors
by: Mónica Martínez-Montiel, et al.
Published: (2023-05-01)

Bis(2,6-di(pyridin-2-yl)pyridin-4-yl)-6,6′-(1,2-diselanediyl)dihexanoate
by: Evelyn Popa, et al.
Published: (2023-12-01)

6-Cyanonaphthalen-2-yl 4-hexylbenzoate
by: Rahman, Md. Lutfor, et al.
Published: (2014)

Design, synthesis, and biological evaluation of piperazine derivatives involved in the 5-HT1AR/BDNF/PKA pathway
by: Hao Zhou, et al.
Published: (2024-12-01)

Microwave assisted synthesis of 2-(4-substituted piperazin-1-yl)-1, 8-naphthyridine-3-carbonitrile as a new class of serotonin 5-HT< sub> 3</sub> receptor antagonists
by: Mahesh, R., et al.
Published: (2004)

Design, Synthesis and 5-HT<sub>1A</sub> Binding Affinity of <i>N</i>-(3-(4-(2-Methoxyphenyl)piperazin-1-yl)propyl)tricyclo[3.3.1.1<sup>3,7</sup>]decan-1-amine and <i>N</i>-(3-(4-(2-Methoxyphenyl)piperazin-1-yl)propyl)-3,5-dimethyl-tricylo[3.3.1.1<sup>3,7</sup>]decan-1-amine
by: Grigoris Zoidis, et al.
Published: (2022-03-01)

Dichlorido(4-methoxy-2-{ 2-(piperazin-4-ium-1-yl)ethyl iminomethyl}pheno late)cadmium
by: Salga, M.S., et al.
Published: (2011)

Evidence for a 5-HT6 receptor-mediated control of midbrain 5-HT neurons
by: Brouard, J
Published: (2016)

Hexachloridobis{mu(2)-2-(piperazin-1-yl)-N- 1-(2-pyridyl)ethylidene etha namine}trizinc dihydrate
by: Gwaram, N.S., et al.
Published: (2011)

2-{ 2-(Piperazin-4-ium-1-yl)ethyliminio methyl}phenolate 0.06-chloride 0.94-perchlorate
by: Reisi, M.R., et al.
Published: (2011)

Synthesis of 6-Aziridineyl and 6-Triazol-yl of D- Glucitol Derivatives
by: Nabil Y. J. Al-Hiti, et al.
Published: (2012-10-01)

Analysis of brain 5-HT function in transgenic mice overexpressing the 5-HT transporter
by: Jennings, K
Published: (2005)

Crystal structure of 1-[2-[6-(4-methoxyphenyl)-3(2H)-pyridazinone- 2-yl]-acetyl]-4-(3-chlorophenyl)piperazine, C23H23ClN4O3
by: İngeç Ş. K., et al.
Published: (2000-03-01)

9,10-Bis[(4-(2-hydroxyethyl)piperazine-1-yl)prop-2-yne-1-yl]anthracene: Synthesis and G-quadruplex Selectivity
by: Giovanni Ribaudo, et al.
Published: (2020-05-01)

6,7-Dichloro-2,3-bis(pyridin-2-yl)quinoxaline
by: Guy Crundwell, et al.
Published: (2015-02-01)

5-HT6 receptor agonism facilitates emotional learning
by: Marcela ePereira, et al.
Published: (2015-09-01)

Crystal structure of piperazine hexafluorosilicate, (C4N2H12)[SiF6]
by: Tang L. Q., et al.
Published: (2001-04-01)

SINTESIS DAN AKTIVITAS ANTIOKSIDAN 3,6-BIS[(4-HIDROKSI-3- METOKSIFENIL)METILIDEN]PIPERAZIN-2,5-DION DAN 3,6-BIS[(4- HIDROKSI-3,5-DIMETILFENIL)METILIDEN]PIPERAZIN-2,5-DION
by: , Broto Santoso, et al.
Published: (2011)

Synthesis of substituted isoindolo[2,1-a]quinoxalin-6-yl–amino and 6-imino-5-yl thiourea derivatives
by: Barbara Parrino, et al.
Published: (2014-09-01)

Novel <i>N</i>-Arylsulfonylindoles Targeted as Ligands of the 5-HT<sub>6</sub> Receptor. Insights on the Influence of C-5 Substitution on Ligand Affinity
by: Loreto Arrieta-Rodríguez, et al.
Published: (2021-06-01)

Anticancer Activities of 9-chloro-6-(piperazin-1-yl)-11H-indeno[1,2-c] quinolin-11-one (SJ10) in Glioblastoma Multiforme (GBM) Chemoradioresistant Cell Cycle-Related Oncogenic Signatures
by: Ntlotlang Mokgautsi, et al.
Published: (2022-01-01)

2-[(3R,6R)-6-Methyl-2,5-dioxomorpholin-3-yl]-N-(propan-2-yl)acetamide
by: Peng-xue Duan, et al.
Published: (2012-03-01)