Literature DB >> 21324684

Quinolizidinone carboxylic acid selective M1 allosteric modulators: SAR in the piperidine series.

Scott D Kuduk1, 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.   

Abstract

SAR study of the piperidine moiety in a series of quinolizidinone carboxylic acid M(1) positive allosteric modulators was examined. While the SAR was generally flat, compounds were identified with high CNS exposure to warrant additional in vivo evaluation.
Copyright © 2011 Elsevier Ltd. All rights reserved.

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Year:  2011        PMID： 21324684     DOI： 10.1016/j.bmcl.2011.01.094

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


  12 in total

1.  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

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.  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 5.  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

6.  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

7.  Drug Design Strategies for GPCR Allosteric Modulators.

Authors:  P Jeffrey Conn; Scott D Kuduk; Darío Doller
Journal:  Annu Rep Med Chem       Date:  2012       Impact factor: 1.059

8.  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

9.  Chemical modification of the M(1) agonist VU0364572 reveals molecular switches in pharmacology and a bitopic binding mode.

Authors:  Gregory J Digby; Thomas J Utley; Atin Lamsal; Christian Sevel; Douglas J Sheffler; Evan P Lebois; Thomas M Bridges; Michael R Wood; Colleen M Niswender; Craig W Lindsley; P Jeffrey Conn
Journal:  ACS Chem Neurosci       Date:  2012-09-09       Impact factor: 4.418

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
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