Literature DB >> 20004574

Parallel synthesis of N-biaryl quinolone carboxylic acids as selective M(1) positive allosteric modulators.

Feng V Yang1, William D Shipe, Jaime L Bunda, M Brad Nolt, David D Wisnoski, Zhijian Zhao, James C Barrow, William J Ray, Lei Ma, Marion Wittmann, Matthew A Seager, Kenneth A Koeplinger, George D Hartman, Craig W Lindsley.   

Abstract

An iterative analog library synthesis approach was employed in the exploration of a quinolone carboxylic acid series of selective M(1) positive allosteric modulators, and strategies for improving potency and plasma free fraction were identified. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 20004574     DOI： 10.1016/j.bmcl.2009.11.100

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


  24 in total

1.  Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Authors:  Bruce J Melancon; Corey R Hopkins; Michael R Wood; Kyle A Emmitte; Colleen M Niswender; Arthur Christopoulos; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2012-01-06       Impact factor: 7.446

2.  Development of a highly selective, orally bioavailable and CNS penetrant M1 agonist derived from the MLPCN probe ML071.

Authors:  Evan P Lebois; Gregory J Digby; Douglas J Sheffler; Bruce J Melancon; James C Tarr; Hyekyung P Cho; Nicole R Miller; Ryan Morrison; Thomas M Bridges; Zixiu Xiang; J Scott Daniels; Michael R Wood; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2011-08-24       Impact factor: 2.823

Review 3.  Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders.

Authors:  Gregory J Digby; Jana K Shirey; P Jeffrey Conn
Journal:  Mol Biosyst       Date:  2010-06-25

4.  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

5.  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

Review 6.  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

7.  Muscarinic Acetylcholine Receptor Subtypes as Potential Drug Targets for the Treatment of Schizophrenia, Drug Abuse and Parkinson's Disease.

Authors:  Ditte Dencker; Morgane Thomsen; Gitta Wörtwein; Pia Weikop; Yinghong Cui; Jongrye Jeon; Jürgen Wess; Anders Fink-Jensen
Journal:  ACS Chem Neurosci       Date:  2012       Impact factor: 4.418

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

Authors:  Zhi-Qiang Yang; Youheng Shu; Lei Ma; Marion Wittmann; William J Ray; Matthew A Seager; Kenneth A Koeplinger; Charles D Thompson; George D Hartman; Mark T Bilodeau; Scott D Kuduk
Journal:  ACS Med Chem Lett       Date:  2014-02-20       Impact factor: 4.345

9.  The discovery of VU0486846: steep SAR from a series of M1 PAMs based on a novel benzomorpholine core.

Authors:  Jeanette L Bertron; Hyekyung P Cho; Pedro M Garcia-Barrantes; Joseph D Panarese; James M Salovich; Kellie D Nance; Darren W Engers; Jerri M Rook; Anna L Blobaum; Colleen M Niswender; Shaun R Stauffer; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2018-05-05       Impact factor: 2.823

10.  Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.

Authors:  Thomas M Bridges; J Phillip Kennedy; Hyekyung P Cho; Micah L Breininger; Patrick R Gentry; Corey R Hopkins; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-11-22       Impact factor: 2.823
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