Literature DB >> 19962304

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

Scott D Kuduk1, 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.   

Abstract

Incorporation of pyridines and diazines into the biphenyl region of quinolone carboxylic acid derived M(1) positive allosteric modulators was investigated as a means of lowering plasma protein binding to enhance CNS exposure. Copyright 2009 Elsevier Ltd. All rights reserved.

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Year:  2009        PMID： 19962304     DOI： 10.1016/j.bmcl.2009.11.059

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


  10 in total

Review 1.  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

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.  The muscarinic M1 receptor positive allosteric modulator PQCA improves cognitive measures in rat, cynomolgus macaque, and rhesus macaque.

Authors:  Jason M Uslaner; Donnie Eddins; Vanita Puri; Christopher E Cannon; Jane Sutcliffe; Chan Sing Chew; Michelle Pearson; Jeffrey A Vivian; Ronald K Chang; William J Ray; Scott D Kuduk; Marion Wittmann
Journal:  Psychopharmacology (Berl)       Date:  2012-07-24       Impact factor: 4.530

Review 4.  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

5.  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

6.  Identification of amides as carboxylic Acid surrogates for quinolizidinone-based m1 positive allosteric modulators.

Authors:  Scott D Kuduk; Ronald K Chang; Thomas J Greshock; 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:  2012-10-13       Impact factor: 4.345

7.  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

8.  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 9.  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

10.  Further exploration of M₁ allosteric agonists: subtle structural changes abolish M₁ allosteric agonism and result in pan-mAChR orthosteric antagonism.

Authors:  Douglas J Sheffler; Christian Sevel; Uyen Le; Kimberly M Lovell; James C Tarr; Sheridan J S Carrington; Hyekyung P Cho; Gregory J Digby; Colleen M Niswender; P Jeffrey Conn; Corey R Hopkins; Michael R Wood; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2012-11-09       Impact factor: 2.823
  10 in total

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