Literature DB >> 24900888

Discovery of naphthyl-fused 5-membered lactams as a new class of m1 positive allosteric modulators.

Zhi-Qiang Yang1, Youheng Shu1, Lei Ma1, Marion Wittmann1, William J Ray1, Matthew A Seager1, Kenneth A Koeplinger1, Charles D Thompson1, George D Hartman1, Mark T Bilodeau1, Scott D Kuduk1.   

Abstract

Selective activation of the M1 muscarinic receptor via positive allosteric modulation represents an original approach to treat the cognitive decline in patients with Alzheimer's disease. A series of naphthyl-fused 5-membered lactams were identified as a new class of M1 positive allosteric modulators and were found to possess good potency and in vivo efficacy.

Entities:  

Keywords:  Alzheimer’s disease; M1; acetylcholine; muscarinic; positive allosteric modulators

Year:  2014        PMID： 24900888      PMCID： PMC4027734          DOI： 10.1021/ml500055h

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


  19 in total

Review 1.  Structural modifications that alter the P-glycoprotein efflux properties of compounds.

Authors:  Stephen A Hitchcock
Journal:  J Med Chem       Date:  2012-04-16       Impact factor: 7.446

2.  Hydroxy cycloalkyl fused pyridone carboxylic acid M(1) positive allosteric modulators.

Authors:  Scott D Kuduk; Robert M DiPardo; Douglas C Beshore; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
Journal:  Bioorg Med Chem Lett       Date:  2010-03-10       Impact factor: 2.823

Review 3.  Development of M1 mAChR allosteric and bitopic ligands: prospective therapeutics for the treatment of cognitive deficits.

Authors:  Briana J Davie; Arthur Christopoulos; Peter J Scammells
Journal:  ACS Chem Neurosci       Date:  2013-05-23       Impact factor: 4.418

Review 4.  The molecular basis of muscarinic receptor diversity.

Authors:  T I Bonner
Journal:  Trends Neurosci       Date:  1989-04       Impact factor: 13.837

Review 5.  New subtypes of muscarinic acetylcholine receptors.

Authors:  T I Bonner
Journal:  Trends Pharmacol Sci       Date:  1989-12       Impact factor: 14.819

6.  Quinolizidinone carboxylic acids as CNS penetrant, selective m1 allosteric muscarinic receptor modulators.

Authors:  Scott D Kuduk; Ronald K Chang; Christina N Di Marco; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau
Journal:  ACS Med Chem Lett       Date:  2010-06-04       Impact factor: 4.345

7.  A selective allosteric potentiator of the M1 muscarinic acetylcholine receptor increases activity of medial prefrontal cortical neurons and restores impairments in reversal learning.

Authors:  Jana K Shirey; Ashley E Brady; Paulianda J Jones; Albert A Davis; Thomas M Bridges; J Phillip Kennedy; Satyawan B Jadhav; Usha N Menon; Zixiu Xiang; Mona L Watson; Edward P Christian; James J Doherty; Michael C Quirk; Dean H Snyder; James J Lah; Allan I Levey; Michelle M Nicolle; Craig W Lindsley; P Jeffrey Conn
Journal:  J Neurosci       Date:  2009-11-11       Impact factor: 6.167

8.  Pyridine containing M(1) positive allosteric modulators with reduced plasma protein binding.

Authors:  Scott D Kuduk; Christina N Di Marco; Victoria Cofre; Daniel R Pitts; William J Ray; Lei Ma; Marion Wittmann; Matthew A Seager; Matthew Seager; Kenneth Koeplinger; Chuck D Thompson; George D Hartman; Mark T Bilodeau
Journal:  Bioorg Med Chem Lett       Date:  2009-12-02       Impact factor: 2.823

9.  Selective activation of the M1 muscarinic acetylcholine receptor achieved by allosteric potentiation.

Authors:  Lei Ma; Matthew A Seager; Matthew Seager; Marion Wittmann; Marlene Jacobson; Denise Bickel; Maryann Burno; Keith Jones; Valerie Kuzmick Graufelds; Guangping Xu; Michelle Pearson; Alexander McCampbell; Renee Gaspar; Paul Shughrue; Andrew Danziger; Christopher Regan; Rose Flick; Danette Pascarella; Susan Garson; Scott Doran; Constantine Kreatsoulas; Lone Veng; Craig W Lindsley; William Shipe; Scott Kuduk; Cyrille Sur; Gene Kinney; Guy R Seabrook; William J Ray
Journal:  Proc Natl Acad Sci U S A       Date:  2009-08-26       Impact factor: 11.205

Review 10.  Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Arthur Christopoulos; Craig W Lindsley
Journal:  Nat Rev Drug Discov       Date:  2009-01       Impact factor: 84.694
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  6 in total

1.  A Novel M1 PAM VU0486846 Exerts Efficacy in Cognition Models without Displaying Agonist Activity or Cholinergic Toxicity.

Authors:  Jerri M Rook; Jeanette L Bertron; Hyekyung P Cho; Pedro M Garcia-Barrantes; Sean P Moran; James T Maksymetz; Kellie D Nance; Jonathan W Dickerson; Daniel H Remke; Sichen Chang; Joel M Harp; Anna L Blobaum; Colleen M Niswender; Carrie K Jones; Shaun R Stauffer; P Jeffrey Conn; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2018-05-08       Impact factor: 4.418

2.  Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.

Authors:  Changho Han; Arindam Chatterjee; Meredith J Noetzel; Joseph D Panarese; Emery Smith; Peter Chase; Peter Hodder; Colleen Niswender; P Jeffrey Conn; Craig W Lindsley; Shaun R Stauffer
Journal:  Bioorg Med Chem Lett       Date:  2014-11-18       Impact factor: 2.823

3.  MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate.

Authors:  Douglas C Beshore; Christina N Di Marco; Ronald K Chang; Thomas J Greshock; Lei Ma; Marion Wittmann; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; Joy Fuerst; George D Hartman; Mark T Bilodeau; William J Ray; Scott D Kuduk
Journal:  ACS Med Chem Lett       Date:  2018-04-30       Impact factor: 4.345

4.  Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.

Authors:  Joseph D Panarese; Hykeyung P Cho; Jeffrey J Adams; Kellie D Nance; Pedro M Garcia-Barrantes; Sichen Chang; Ryan D Morrison; Anna L Blobaum; Colleen M Niswender; Shaun R Stauffer; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2016-04-29       Impact factor: 2.823

Review 5.  Drug Design Targeting the Muscarinic Receptors and the Implications in Central Nervous System Disorders.

Authors:  Chad R Johnson; Brian D Kangas; Emily M Jutkiewicz; Jack Bergman; Andrew Coop
Journal:  Biomedicines       Date:  2022-02-07

6.  Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M1.

Authors:  Paul K Spearing; Hyekyung P Cho; Vincent B Luscombe; Anna L Blobaum; Olivier Boutaud; Darren W Engers; Alice L Rodriguez; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley; Aaron M Bender
Journal:  Bioorg Med Chem Lett       Date:  2021-06-09       Impact factor: 2.940
  6 in total

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