Literature DB >> 20347302

Peripheral site acetylcholinesterase inhibitors targeting both inflammation and cholinergic dysfunction.

Sherri Young1, Karine Fabio, Christophe Guillon, Pramod Mohanta, Timothy A Halton, Diane E Heck, Robert A Flowers, Jeffrey D Laskin, Ned D Heindel.   

Abstract

The design and study of two classes of noncompetitive acetylcholinesterase inhibitors (AChEIs) which also function as NSAID prodrugs are reported. The most potent AChEIs disclosed contain an aromatic alkyl-aryl linker between an NSAID and a lipophilic choline mimic and they inhibit acetylcholinesterase (AChE) in the submicromolar range. These agents have the therapeutic potential to dually target inflammation by releasing an NSAID in vivo and activating the cholinergic anti-inflammatory pathway via cholinergic up-regulation. 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20347302      PMCID： PMC2864113          DOI： 10.1016/j.bmcl.2010.02.102

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  22 in total

Review 1.  Molecular dynamics of acetylcholinesterase.

Authors:  Tongye Shen; Kaihsu Tai; Richard H Henchman; J Andrew McCammon
Journal:  Acc Chem Res       Date:  2002-06       Impact factor: 22.384

2.  A new and rapid colorimetric determination of acetylcholinesterase activity.

Authors:  G L ELLMAN; K D COURTNEY; V ANDRES; R M FEATHER-STONE
Journal:  Biochem Pharmacol       Date:  1961-07       Impact factor: 5.858

Review 3.  The inflammatory reflex.

Authors:  Kevin J Tracey
Journal:  Nature       Date:  2002 Dec 19-26       Impact factor: 49.962

4.  Synthesis and biological evaluation of omega-(N,N,N-trialkylammonium)alkyl esters and thioesters of carboxylic acid nonsteroidal antiinflammatory agents.

Authors:  M C Venuti; J M Young; P J Maloney; D Johnson; K McGreevy
Journal:  Pharm Res       Date:  1989-10       Impact factor: 4.200

5.  Bifunctional compounds eliciting anti-inflammatory and anti-cholinesterase activity as potential treatment of nerve and blister chemical agents poisoning.

Authors:  Gabi Amitai; Rachel Adani; Eliezer Fishbein; Haim Meshulam; Ido Laish; Shlomit Dachir
Journal:  J Appl Toxicol       Date:  2006 Jan-Feb       Impact factor: 3.446

6.  Potent acetylcholinesterase inhibitors: design, synthesis and structure-activity relationships of alkylene linked bis-galanthamine and galanthamine-galanthaminium salts.

Authors:  C Guillou; A Mary; D Z Renko; E Gras; C Thal
Journal:  Bioorg Med Chem Lett       Date:  2000-04-03       Impact factor: 2.823

7.  Bifunctional compounds eliciting both anti-inflammatory and cholinergic activity as potential drugs for neuroinflammatory impairments.

Authors:  Eran Nizri; Rellie Adani; Haim Meshulam; Gabi Amitai; Talma Brenner
Journal:  Neurosci Lett       Date:  2004-12-08       Impact factor: 3.046

Review 8.  The link between inflammation, synaptic transmission and neurodegeneration in multiple sclerosis.

Authors:  D Centonze; L Muzio; S Rossi; R Furlan; G Bernardi; G Martino
Journal:  Cell Death Differ       Date:  2009-11-20       Impact factor: 15.828

9.  Synthesis, biological activity, and docking studies of new acetylcholinesterase inhibitors of the bispyridinium type.

Authors:  Petra Kapková; Nikolaus Stiefl; Ulf Sürig; Bernd Engels; Knut Baumann; Ulrike Holzgrabe
Journal:  Arch Pharm (Weinheim)       Date:  2003-11       Impact factor: 3.751

10.  Effects of charge, volume, and surface on binding of inhibitor and substrate moieties to acetylcholinesterase.

Authors:  S G Cohen; S B Chishti; J L Elkind; H Reese; J B Cohen
Journal:  J Med Chem       Date:  1985-09       Impact factor: 7.446
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  9 in total

1.  Investigation of anticholinergic and non-steroidal anti-inflammatory prodrugs which reduce chemically induced skin inflammation.

Authors:  Sherri C Young; Karine M Fabio; Mou-Tuan Huang; Jaya Saxena; Meredith P Harman; Christophe D Guillon; Anna M Vetrano; Diane E Heck; Robert A Flowers; Ned D Heindel; Jeffrey D Laskin
Journal:  J Appl Toxicol       Date:  2011-02-11       Impact factor: 3.446

2.  Ethynylphenyl carbonates and carbamates as dual-action acetylcholinesterase inhibitors and anti-inflammatory agents.

Authors:  Jaya Saxena; David Meloni; Mou-Tuan Huang; Diane E Heck; Jeffrey D Laskin; Ned D Heindel; Sherri C Young
Journal:  Bioorg Med Chem Lett       Date:  2015-10-23       Impact factor: 2.823

3.  Therapeutic potential of a non-steroidal bifunctional anti-inflammatory and anti-cholinergic agent against skin injury induced by sulfur mustard.

Authors:  Yoke-Chen Chang; James D Wang; Rita A Hahn; Marion K Gordon; Laurie B Joseph; Diane E Heck; Ned D Heindel; Sherri C Young; Patrick J Sinko; Robert P Casillas; Jeffrey D Laskin; Debra L Laskin; Donald R Gerecke
Journal:  Toxicol Appl Pharmacol       Date:  2014-08-13       Impact factor: 4.219

4.  Sulfur mustard induced mast cell degranulation in mouse skin is inhibited by a novel anti-inflammatory and anticholinergic bifunctional prodrug.

Authors:  Laurie B Joseph; Gabriella M Composto; Roberto M Perez; Hong-Duck Kim; Robert P Casillas; Ned D Heindel; Sherri C Young; Carl J Lacey; Jaya Saxena; Christophe D Guillon; Claire R Croutch; Jeffrey D Laskin; Diane E Heck
Journal:  Toxicol Lett       Date:  2017-11-07       Impact factor: 4.372

5.  Back-scattering interferometry: an ultrasensitive method for the unperturbed detection of acetylcholinesterase-inhibitor interactions.

Authors:  Gabrielle L Haddad; Sherri C Young; Ned D Heindel; Darryl J Bornhop; Robert A Flowers
Journal:  Angew Chem Int Ed Engl       Date:  2012-10-04       Impact factor: 15.336

Review 6.  Multi-inhibitor prodrug constructs for simultaneous delivery of anti-inflammatory agents to mustard-induced skin injury.

Authors:  Carl J Lacey; Irene Wohlman; Christophe Guillon; Jaya Saxena; Cynthia Fianu-Velgus; Erik Aponte; Sherri C Young; Diane E Heck; Laurie B Joseph; Jeffrey D Laskin; Ned D Heindel
Journal:  Ann N Y Acad Sci       Date:  2016-08-09       Impact factor: 5.691

7.  Mitigation of nitrogen mustard mediated skin injury by a novel indomethacin bifunctional prodrug.

Authors:  Gabriella M Composto; Jeffrey D Laskin; Debra L Laskin; Donald R Gerecke; Robert P Casillas; Ned D Heindel; Laurie B Joseph; Diane E Heck
Journal:  Exp Mol Pathol       Date:  2016-05-14       Impact factor: 3.362

Review 8.  Prodrugs of nonsteroidal anti-inflammatory drugs (NSAIDs), more than meets the eye: a critical review.

Authors:  Amjad M Qandil
Journal:  Int J Mol Sci       Date:  2012-12-17       Impact factor: 5.923

9.  Acetylcholinesterase inhibitors reduce neuroinflammation and -degeneration in the cortex and hippocampus of a surgery stress rat model.

Authors:  Alexander Kalb; Clarissa von Haefen; Marco Sifringer; Annalena Tegethoff; Nadine Paeschke; Mariya Kostova; Aarne Feldheiser; Claudia D Spies
Journal:  PLoS One       Date:  2013-05-03       Impact factor: 3.240
  9 in total

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