Extended N-Arylsulfonylindoles as 5-HT6 Receptor Antagonists: Design, Synthesis & Biological Evaluation

Extended N-Arylsulfonylindoles as 5-HT6 Receptor Antagonists: Design, Synthesis & Biological Evaluation

Based on a known pharmacophore model for 5-HT6 receptor antagonists, a series of novel extended derivatives of the N-arylsulfonyindole scaffold were designed and identified as a new class of 5-HT6 receptor modulators. Eight of the compounds exhibited moderate to high binding affinities and displayed...

Cur síos iomlán

Sonraí bibleagrafaíochta
Príomhchruthaitheoirí:	Gonzalo Vera, Carlos F. Lagos, Sebastián Almendras, Dan Hebel, Francisco Flores, Gissella Valle-Corvalán, C. David Pessoa-Mahana, Jaime Mella-Raipán, Rodrigo Montecinos, Gonzalo Recabarren-Gajardo
Formáid:	Alt
Teanga:	English
Foilsithe / Cruthaithe:	MDPI AG 2016-08-01
Sraith:	Molecules
Ábhair:	arylsulfonylindole 5-HT6 receptor antagonists binding affinity arylpiperazines
Rochtain ar líne:	http://www.mdpi.com/1420-3049/21/8/1070

Míreanna comhchosúla

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
de réir: Loreto Arrieta-Rodríguez, et al.
Foilsithe / Cruthaithe: (2021-06-01)

Design of an innovative nanovehicle to enhance brain permeability of a novel 5-HT6 receptor antagonist
de réir: María Javiera Alvarez-Figueroa, et al.
Foilsithe / Cruthaithe: (2024-12-01)

Synthesis and Bioactivity Evaluation of N-Arylsulfonylindole Analogs Bearing a Rhodanine Moiety as Antibacterial Agents
de réir: Ming-Xia Song, et al.
Foilsithe / Cruthaithe: (2017-06-01)

Synthesis, Docking Studies and Biological Evaluation of Benzo[b]thiophen-2-yl-3-(4-arylpiperazin-1-yl)-propan-1-one Derivatives on 5-HT1A Serotonin Receptors
de réir: Ramiro Araya-Maturana, et al.
Foilsithe / Cruthaithe: (2012-02-01)

Influence of N–1 substituent properties on binding affinities of arylpiperazines to the binding site of 5-HT1A receptor
de réir: MARIO V. ZLATOVIC, et al.
Foilsithe / Cruthaithe: (2006-11-01)

Influence of N-1 substituent properties on binding affinities of arylpiperazines to the binding site of 5-HT1A receptor
de réir: Zlatović Mario V., et al.
Foilsithe / Cruthaithe: (2006-01-01)

Synthesis, computational studies and preliminary pharmacological evaluation of 2-[4-(aryl substituted) piperazin-1-yl]-N-benzylacetamides as potential antipsychotics
de réir: Sushil Kumar, et al.
Foilsithe / Cruthaithe: (2016-11-01)

New, Eco-Friendly Method for Synthesis of 3-Chlorophenyl and 1,1′-Biphenyl Piperazinylhexyl Trazodone Analogues with Dual 5-HT<sub>1A</sub>/5-HT<sub>7</sub> Affinity and Its Antidepressant-like Activity
de réir: Przemysław Zaręba, et al.
Foilsithe / Cruthaithe: (2022-10-01)

Mechanism Exploration of Arylpiperazine Derivatives Targeting the 5-HT2A Receptor by In Silico Methods
de réir: Feng Lin, et al.
Foilsithe / Cruthaithe: (2017-06-01)

5-HT3 receptor antagonists protect against pressure overload-induced cardiac hypertrophy in murine
de réir: Rong Huo, et al.
Foilsithe / Cruthaithe: (2012-02-01)

Synthesis, computational and pharmacological evaluation of novel N-{4-[2-(4-aryl-piperazin-1-yl)ethyl]phenyl}-arylamides
de réir: Andrić Deana B., et al.
Foilsithe / Cruthaithe: (2024-01-01)

3D-QSAR modeling and pharmacophore study of serotonin 5HT-₂A receptors antagonists
de réir: Antonijević Mirjana, et al.
Foilsithe / Cruthaithe: (2017-01-01)

Structural determinants influencing halogen bonding: a case study on azinesulfonamide analogs of aripiprazole as 5-HT1A, 5-HT7, and D2 receptor ligands
de réir: Krzysztof Marciniec, et al.
Foilsithe / Cruthaithe: (2018-05-01)

5-HT3 receptor antagonists decrease the prevalence of postoperative delirium in older patients undergoing orthopedic lower limb surgery
de réir: Hyun-Jung Shin, et al.
Foilsithe / Cruthaithe: (2021-12-01)

Discovery and Structure-Based Optimization of 6-Bromotryptamine Derivatives as Potential 5-HT2A Receptor Antagonists
de réir: Lijian Ding, et al.
Foilsithe / Cruthaithe: (2015-09-01)

Dexamethasone-sparing strategies in anthracycline and cyclophosphamide-based chemotherapy with a focus on 5-HT3 receptor antagonists: a network meta-analysis
de réir: Daichi Watanabe, et al.
Foilsithe / Cruthaithe: (2024-07-01)

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

Investigation of key interactions between the second extracellular loop of dopamine D2 receptor and several hydroxy-N-{[2-(4-phenyl-piperaziny-1-yl)ethyl]phenyl}-nicotinamides
de réir: Šukalović Vladimir, et al.
Foilsithe / Cruthaithe: (2014-01-01)

HEMORHEOLOGICAL PROPERTIES OF THE 5-HT2A-ANTAGONIST OF THE 2-METHOXYPHENYL-IMIDAZOBENZIMIDAZOLE DERIVATIVE OF THE RU-31 COMPOUND AND CYPROHEPTADINE, IN COMPARISON WITH PENTHOXYPHYLLINE
de réir: D. S. Yakovlev, et al.
Foilsithe / Cruthaithe: (2021-03-01)

Pharmacological evaluation of novel 5-HT 3 receptor antagonist, QCM-13 (N-cyclohexyl-3-methoxyquinoxalin-2-carboxamide) as anti-anxiety agent in behavioral test battery
de réir: Deepali Gupta, et al.
Foilsithe / Cruthaithe: (2015-01-01)

Microwave-Assisted Synthesis of Trazodone and Its Derivatives as New 5-HT<sub>1A</sub> Ligands: Binding and Docking Studies
de réir: Jolanta Jaśkowska, et al.
Foilsithe / Cruthaithe: (2019-04-01)

Design, Synthesis and Biological Evaluation of Novel N-Arylpiperazines Containing a 4,5-Dihydrothiazole Ring
de réir: Giorgia Andreozzi, et al.
Foilsithe / Cruthaithe: (2023-10-01)

Synthesis and biological evaluation of 5-substituted derivatives of benzimidazole
de réir: Vasić Vesna P., et al.
Foilsithe / Cruthaithe: (2014-01-01)

Design, Synthesis, Binding and Docking-Based 3D-QSAR Studies of 2-Pyridylbenzimidazoles—A New Family of High Affinity CB1 Cannabinoid Ligands
de réir: Patricio Iturriaga-Vásquez, et al.
Foilsithe / Cruthaithe: (2013-04-01)

Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT2A and 5-HT2B serotonin receptors
de réir: Prithvi Hemanth, et al.
Foilsithe / Cruthaithe: (2023-01-01)

The affinity and selectivity of α‐adrenoceptor antagonists, antidepressants and antipsychotics for the human α2A, α2B, and α2C‐adrenoceptors and comparison with human α1 and β‐adrenoceptors
de réir: Richard G.W. Proudman, et al.
Foilsithe / Cruthaithe: (2022-04-01)

Design, Sustainable Synthesis and Biological Evaluation of a Novel Dual α2A/5-HT7 Receptor Antagonist with Antidepressant-Like Properties
de réir: Vittorio Canale, et al.
Foilsithe / Cruthaithe: (2021-06-01)

Arylpiperazine Derivatives and Cancer: A New Challenge in Medicinal Chemistry
de réir: Giorgia Andreozzi, et al.
Foilsithe / Cruthaithe: (2024-10-01)

Modeling key interactions between dopamine D2 receptor second extracellular loop and arylpiperazine ligands
de réir: Šukalović Vladimir, et al.
Foilsithe / Cruthaithe: (2012-01-01)

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
de réir: Grigoris Zoidis, et al.
Foilsithe / Cruthaithe: (2022-03-01)

Synthesis, bioactivity, and molecular docking of novel arylpiperazine derivatives as potential AR antagonists
de réir: Yueheng Qi, et al.
Foilsithe / Cruthaithe: (2022-08-01)

A new approach to ‘on-demand’ treatment of lifelong premature ejaculation by treatment with a combination of a 5-HT1A receptor antagonist and SSRI in rats
de réir: Jocelien D. A. Olivier, et al.
Foilsithe / Cruthaithe: (2023-09-01)

Antiemetic Prophylaxis with Fosaprepitant and 5-HT3-Receptor Antagonists in Pediatric Patients Undergoing Autologous Hematopoietic Stem Cell Transplantation
de réir: Cabanillas Stanchi KM, et al.
Foilsithe / Cruthaithe: (2020-09-01)

6-[2-(4-Arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2H-benzimidazole-2-thiones: synthesis and pharmacological evaluation
de réir: DEANA ANDRIC, et al.
Foilsithe / Cruthaithe: (2007-08-01)

6-[2-(4-arylpiperazin-1-yl)ethyl]-4-halo-1,3-dihydro-2h-benzimidazole-2-thiones: Synthesis and pharmacological evaluation
de réir: Andrić Deana, et al.
Foilsithe / Cruthaithe: (2007-01-01)

Synthesis of novel 2-(piperazino-1-yl-alkyl)-1H-benzimidazole derivates and assessment of their interactions with the D2 dopamine receptor
de réir: Penjišević Jelena Z., et al.
Foilsithe / Cruthaithe: (2019-01-01)

Synthesis and pharmacological evaluation of several N-(2-nitrophenyl)piperazine derivatives
de réir: DEANA ANDRIC, et al.
Foilsithe / Cruthaithe: (2007-05-01)

Investigation of antibacterial activity of cinnamyl derivatives of arylpiperazine
de réir: Novaković Irena, et al.
Foilsithe / Cruthaithe: (2012-01-01)

Azologization of serotonin 5-HT3 receptor antagonists
de réir: Karin Rustler, et al.
Foilsithe / Cruthaithe: (2019-03-01)

Structure-Activity Relationships of Substituted 2,3,4,4a,5,10b-Hexahydro-benz[h]isoquinoline-6(1H)-ones as 5-HT2c Receptor Antagonists
de réir: Heinz Stadler, et al.
Foilsithe / Cruthaithe: (2000-11-01)