Literature DB >> 18178088

Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists.

L Michelle Lewis1, Douglas Sheffler, Richard Williams, Thomas M Bridges, J Phillip Kennedy, J T Brogan, Matthew J Mulder, Lyndsey Williams, Natalia T Nalywajko, Colleen M Niswender, Charles D Weaver, P Jeffrey Conn, Craig W Lindsley.   

Abstract

This Letter describes the synthesis and SAR, developed through an iterative analogue library approach, of a novel series of selective M1 mAChR antagonists for the potential treatment of Parkinson's disease, dystonia and other movement disorders. Compounds in this series possess M1 antagonist IC(50)s in the 441nM-19microM range with 8- to >340-fold functional selectivity versus rM2-rM5.

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Year:  2008        PMID： 18178088      PMCID： PMC2275053          DOI： 10.1016/j.bmcl.2007.12.051

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


  16 in total

Review 1.  Muscarinic receptor ligands and their therapeutic potential.

Authors:  R M Eglen; A Choppin; M P Dillon; S Hegde
Journal:  Curr Opin Chem Biol       Date:  1999-08       Impact factor: 8.822

2.  Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries.

Authors:  William Leister; Kimberly Strauss; David Wisnoski; Zhijian Zhao; Craig Lindsley
Journal:  J Comb Chem       Date:  2003 May-Jun

3.  Effects of xanomeline, a selective muscarinic receptor agonist, on cognitive function and behavioral symptoms in Alzheimer disease.

Authors:  N C Bodick; W W Offen; A I Levey; N R Cutler; S G Gauthier; A Satlin; H E Shannon; G D Tollefson; K Rasmussen; F P Bymaster; D J Hurley; W Z Potter; S M Paul
Journal:  Arch Neurol       Date:  1997-04

4.  The relative selectivity of anticholinergic drugs for the M1 and M2 muscarinic receptor subtypes.

Authors:  R E Burke
Journal:  Mov Disord       Date:  1986       Impact factor: 10.338

5.  Identification of a family of muscarinic acetylcholine receptor genes.

Authors:  T I Bonner; N J Buckley; A C Young; M R Brann
Journal:  Science       Date:  1987-07-31       Impact factor: 47.728

6.  Subtype-selective positive cooperative interactions between brucine analogs and acetylcholine at muscarinic receptors: functional studies.

Authors:  N J Birdsall; T Farries; P Gharagozloo; S Kobayashi; S Lazareno; M Sugimoto
Journal:  Mol Pharmacol       Date:  1999-04       Impact factor: 4.436

Review 7.  Muscarinic toxins from the green mamba.

Authors:  K N Bradley
Journal:  Pharmacol Ther       Date:  2000-02       Impact factor: 12.310

8.  Synthesis, affinity profile, and functional activity of muscarinic antagonists with a 1-methyl-2-(2,2-alkylaryl-1,3-oxathiolan-5-yl)pyrrolidine structure.

Authors:  Silvia Dei; Cristina Bellucci; Michela Buccioni; Marta Ferraroni; Luca Guandalini; Dina Manetti; Elisabetta Martini; Gabriella Marucci; Rosanna Matucci; Marta Nesi; Maria Novella Romanelli; Serena Scapecchi; Elisabetta Teodori
Journal:  J Med Chem       Date:  2007-02-17       Impact factor: 7.446

9.  The selective muscarinic agonist xanomeline improves both the cognitive deficits and behavioral symptoms of Alzheimer disease.

Authors:  N C Bodick; W W Offen; H E Shannon; J Satterwhite; R Lucas; R van Lier; S M Paul
Journal:  Alzheimer Dis Assoc Disord       Date:  1997       Impact factor: 2.703

10.  Pirenzepine distinguishes between different subclasses of muscarinic receptors.

Authors:  R Hammer; C P Berrie; N J Birdsall; A S Burgen; E C Hulme
Journal:  Nature       Date:  1980-01-03       Impact factor: 49.962
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  8 in total

1.  A novel selective muscarinic acetylcholine receptor subtype 1 antagonist reduces seizures without impairing hippocampus-dependent learning.

Authors:  Douglas J Sheffler; Richard Williams; Thomas M Bridges; Zixiu Xiang; Alexander S Kane; Nellie E Byun; Satyawan Jadhav; Mathew M Mock; Fang Zheng; L Michelle Lewis; Carrie K Jones; Colleen M Niswender; Charles D Weaver; Craig W Lindsley; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2009-04-30       Impact factor: 4.436

Review 2.  NIMH initiatives to facilitate collaborations among industry, academia, and government for the discovery and clinical testing of novel models and drugs for psychiatric disorders.

Authors:  Linda S Brady; Lois Winsky; Wayne Goodman; Mary Ellen Oliveri; Ellen Stover
Journal:  Neuropsychopharmacology       Date:  2008-09-17       Impact factor: 7.853

3.  Synthesis and SAR of N-(4-(4-alklylpiperazin-1-yl)phenyl)benzamides as muscarinic acetylcholine receptor subtype 1 (M1) anatgonists.

Authors:  Nicole R Miller; R Nathan Daniels; David Lee; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2010-02-13       Impact factor: 2.823

4.  In Silico Studies Targeting G-protein Coupled Receptors for Drug Research Against Parkinson's Disease.

Authors:  Agostinho Lemos; Rita Melo; Antonio Jose Preto; Jose Guilherme Almeida; Irina Sousa Moreira; Maria Natalia Dias Soeiro Cordeiro
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363

Review 5.  The neurobiological basis for novel experimental therapeutics in dystonia.

Authors:  Anthony M Downs; Kaitlyn M Roman; Simone A Campbell; Antonio Pisani; Ellen J Hess; Paola Bonsi
Journal:  Neurobiol Dis       Date:  2019-07-04       Impact factor: 5.996

6.  MAOS ls for the general synthesis and lead optimization of 3,6-disubstituted-[1,2,4]triazolo[4,3-b]pyridazines.

Authors:  Leslie N Aldrich; Evan P Lebois; L Michelle Lewis; Natalia T Nalywajko; Colleen M Niswender; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Tetrahedron Lett       Date:  2009-01-14       Impact factor: 2.415

7.  Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.

Authors:  Alice L Rodriguez; Richard Williams; Ya Zhou; Stacey R Lindsley; Uyen Le; Mark D Grier; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-05-03       Impact factor: 2.823

8.  Synthesis and biological characterization of a series of novel diaryl amide M₁ antagonists.

Authors:  Michael S Poslusney; Christian Sevel; Thomas J Utley; Thomas M Bridges; Ryan D Morrison; Nathan R Kett; Douglas J Sheffler; Colleen M Niswender; J S Daniels; P J Conn; Craig W Lindsley; Michael R Wood
Journal:  Bioorg Med Chem Lett       Date:  2012-09-23       Impact factor: 2.823
  8 in total

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