Literature DB >> 24900216

Novel and Potent 5-Piperazinyl Methyl-N 1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands.

Ramakrishna V S Nirogi1, Prabhakar Kothmirkar1, Ramasastri Kambhampati1, Jagadish Babu Konda1, Sobhanadri Arepalli1, Narasimhareddy G Pamuleti1, Amol D Deshpande1, Trinathreddy Bandyala1, Anil K Shinde1, P K Dubey2.   

Abstract

The exclusive distribution of 5-HT6 receptors in the brain regions associated with learning and memory makes it an ideal target for cognitive disorders. A novel series of 5-piperazinyl methyl-N 1-aryl sulfonyl indoles were designed and synthesized as 5-HT6R ligands. Most of the synthesized compounds are potent when tested by in vitro radioligand binding assay. The lead compound from the series does not have the CYP liabilities and is active in an animal model of cognition.

Entities:  

Keywords:  5-HT6R; 5-Piperazinyl methyl-N1-aryl sulfonyl indole; Morris water mazes; NORT; PK profile; SAR

Year:  2010        PMID： 24900216      PMCID： PMC4007800          DOI： 10.1021/ml100101u

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  16 in total

Review 1.  An update on the role of the 5-hydroxytryptamine6 receptor in cognitive function.

Authors:  Kevin C F Fone
Journal:  Neuropharmacology       Date:  2008-07-04       Impact factor: 5.250

2.  N-Arylsulfonylindole derivatives as serotonin 5-HT(6) receptor ligands.

Authors:  M G Russell; R J Baker; L Barden; M S Beer; L Bristow; H B Broughton; M Knowles; G McAllister; S Patel; J L Castro
Journal:  J Med Chem       Date:  2001-11-08       Impact factor: 7.446

3.  N1-(Benzenesulfonyl)tryptamines as novel 5-HT6 antagonists.

Authors:  Y Tsai; M Dukat; A Slassi; N MacLean; L Demchyshyn; J E Savage; B L Roth; S Hufesein; M Lee; R A Glennon
Journal:  Bioorg Med Chem Lett       Date:  2000-10-16       Impact factor: 2.823

4.  The 5-hydroxytryptamine6 receptor-selective radioligand [3H]Ro 63-0563 labels 5-hydroxytryptamine receptor binding sites in rat and porcine striatum.

Authors:  F G Boess; C Riemer; M Bös; J Bentley; A Bourson; A J Sleight
Journal:  Mol Pharmacol       Date:  1998-09       Impact factor: 4.436

5.  The effects of neurotoxic lesions of the perirhinal cortex combined to fornix transection on object recognition memory in the rat.

Authors:  A Ennaceur; J P Aggleton
Journal:  Behav Brain Res       Date:  1997-11       Impact factor: 3.332

6.  N1-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT6 receptor antagonists.

Authors:  Derek C Cole; John W Ellingboe; William J Lennox; Hossein Mazandarani; Deborah L Smith; Joseph R Stock; Guoming Zhang; Ping Zhou; Lee E Schechter
Journal:  Bioorg Med Chem Lett       Date:  2005-01-17       Impact factor: 2.823

7.  Binding of serotonin and N1-benzenesulfonyltryptamine-related analogs at human 5-HT6 serotonin receptors: receptor modeling studies.

Authors:  Małgorzata Dukat; Philip D Mosier; Renata Kolanos; Bryan L Roth; Richard A Glennon
Journal:  J Med Chem       Date:  2008-01-18       Impact factor: 7.446

8.  Characterization of Ro 04-6790 and Ro 63-0563: potent and selective antagonists at human and rat 5-HT6 receptors.

Authors:  A J Sleight; F G Boess; M Bös; B Levet-Trafit; C Riemer; A Bourson
Journal:  Br J Pharmacol       Date:  1998-06       Impact factor: 8.739

9.  5-Chloro-N-(4-methoxy-3-piperazin-1-yl- phenyl)-3-methyl-2-benzothiophenesulfon- amide (SB-271046): a potent, selective, and orally bioavailable 5-HT6 receptor antagonist.

Authors:  S M Bromidge; A M Brown; S E Clarke; K Dodgson; T Gager; H L Grassam; P M Jeffrey; G F Joiner; F D King; D N Middlemiss; S F Moss; H Newman; G Riley; C Routledge; P Wyman
Journal:  J Med Chem       Date:  1999-01-28       Impact factor: 7.446

Review 10.  The serotonin 5-HT6 receptor: a viable drug target for treating cognitive deficits in Alzheimer's disease.

Authors:  Werner J Geldenhuys; Cornelis J Van der Schyf
Journal:  Expert Rev Neurother       Date:  2009-07       Impact factor: 4.618
View more
  1 in total

Review 1.  Role of serotonin in Alzheimer's disease: a new therapeutic target?

Authors:  Werner J Geldenhuys; Cornelis J Van der Schyf
Journal:  CNS Drugs       Date:  2011-09-01       Impact factor: 5.749
  1 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.