Literature DB >> 15658848

Discovery of 5-arylsulfonamido-3-(pyrrolidin-2-ylmethyl)-1H-indole derivatives as potent, selective 5-HT6 receptor agonists and antagonists.

Derek C Cole1, William J Lennox, Sabrina Lombardi, John W Ellingboe, Ronald C Bernotas, Gregory J Tawa, Hossein Mazandarani, Deborah L Smith, Guoming Zhang, Joseph Coupet, Lee E Schechter.   

Abstract

5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT(6) receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC(50) values of 1 nM or less and functioning as full agonists while the (S)-enantiomers displayed moderate antagonist activity.

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Year:  2005        PMID： 15658848     DOI： 10.1021/jm049243i

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  13 in total

1.  Palladium(II)-catalyzed enantio- and diastereoselective synthesis of pyrrolidine derivatives.

Authors:  Ranjan Jana; Tejas P Pathak; Katrina H Jensen; Matthew S Sigman
Journal:  Org Lett       Date:  2012-08-08       Impact factor: 6.005

Review 2.  Alzheimer's disease and age-related memory decline (preclinical).

Authors:  Alvin V Terry; Patrick M Callahan; Brandon Hall; Scott J Webster
Journal:  Pharmacol Biochem Behav       Date:  2011-02-24       Impact factor: 3.533

3.  Synthesis and cross-coupling of sulfonamidomethyltrifluoroborates.

Authors:  Gary A Molander; Nicolas Fleury-Brégeot; Marie-Aude Hiebel
Journal:  Org Lett       Date:  2011-03-02       Impact factor: 6.005

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

Authors:  Ramakrishna V S Nirogi; Prabhakar Kothmirkar; Ramasastri Kambhampati; Jagadish Babu Konda; Sobhanadri Arepalli; Narasimhareddy G Pamuleti; Amol D Deshpande; Trinathreddy Bandyala; Anil K Shinde; P K Dubey
Journal:  ACS Med Chem Lett       Date:  2010-06-24       Impact factor: 4.345

5.  E-6801, a 5-HT6 receptor agonist, improves recognition memory by combined modulation of cholinergic and glutamatergic neurotransmission in the rat.

Authors:  Ian Kendall; Helge A Slotten; Xavier Codony; Javier Burgueño; Peter J Pauwels; Jose M Vela; Kevin C F Fone
Journal:  Psychopharmacology (Berl)       Date:  2010-04-20       Impact factor: 4.530

6.  Copper-catalyzed enantioselective intramolecular alkene amination/intermolecular Heck-type coupling cascade.

Authors:  Timothy W Liwosz; Sherry R Chemler
Journal:  J Am Chem Soc       Date:  2012-01-24       Impact factor: 15.419

Review 7.  Serotonin 5-HT6 Receptor Antagonists in Alzheimer's Disease: Therapeutic Rationale and Current Development Status.

Authors:  Hilda Ferrero; Maite Solas; Paul T Francis; Maria J Ramirez
Journal:  CNS Drugs       Date:  2017-01       Impact factor: 5.749

8.  Asymmetric palladium-catalyzed carboamination reactions for the synthesis of enantiomerically enriched 2-(arylmethyl)- and 2-(alkenylmethyl)pyrrolidines.

Authors:  Duy N Mai; John P Wolfe
Journal:  J Am Chem Soc       Date:  2010-09-08       Impact factor: 15.419

9.  Recent Developments in Pd-Catalyzed Alkene Aminoarylation Reactions for the Synthesis of Nitrogen Heterocycles.

Authors:  Danielle M Schultz; John P Wolfe
Journal:  Synthesis (Stuttg)       Date:  2012       Impact factor: 3.157

10.  Enantioselective thiourea-catalyzed intramolecular cope-type hydroamination.

Authors:  Adam R Brown; Christopher Uyeda; Carolyn A Brotherton; Eric N Jacobsen
Journal:  J Am Chem Soc       Date:  2013-04-24       Impact factor: 15.419
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