Literature DB >> 20801651

Heterobiaryl and heterobiaryl ether derived M5 positive allosteric modulators.

Thomas M Bridges1, J Phillip Kennedy, Corey R Hopkins, P Jeffrey Conn, Craig W Lindsley.   

Abstract

This Letter describes a chemical lead optimization campaign directed at VU0238429, the first M(5)-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan G(q) mAChR M(1), M(3), M(5) PAM. An iterative parallel synthesis approach was employed to incorporate basic heterocycles to improve physiochemical properties. Copyright (c) 2010 Elsevier Ltd. All rights reserved.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20801651      PMCID： PMC3179183          DOI： 10.1016/j.bmcl.2010.08.042

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


  19 in total

1.  Discovery and characterization of novel subtype-selective allosteric agonists for the investigation of M(1) receptor function in the central nervous system.

Authors:  Evan P Lebois; Thomas M Bridges; L Michelle Lewis; Eric S Dawson; Alexander S Kane; Zixiu Xiang; Satyawan B Jadhav; Huiyong Yin; J Phillip Kennedy; Jens Meiler; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; C David Weaver; Craig W Lindsley
Journal:  ACS Chem Neurosci       Date:  2010       Impact factor: 4.418

2.  Synthesis and SAR of analogues of the M1 allosteric agonist TBPB. Part I: Exploration of alternative benzyl and privileged structure moieties.

Authors:  Thomas M Bridges; Ashley E Brady; J Phillip Kennedy; R Nathan Daniels; Nicole R Miller; Kwango Kim; Micah L Breininger; Patrick R Gentry; John T Brogan; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2008-09-10       Impact factor: 2.823

Review 3.  Recent progress in the development of mGluR4 positive allosteric modulators for the treatment of Parkinson's disease.

Authors:  Craig W Lindsley; Colleen M Niswender; Darren W Engers; Corey R Hopkins
Journal:  Curr Top Med Chem       Date:  2009       Impact factor: 3.295

4.  3-Cyano-5-fluoro-N-arylbenzamides as negative allosteric modulators of mGlu(5): Identification of easily prepared tool compounds with CNS exposure in rats.

Authors:  Andrew S Felts; Stacey R Lindsley; Jeffrey P Lamb; Alice L Rodriguez; Usha N Menon; Satyawan Jadhav; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Kyle A Emmitte
Journal:  Bioorg Med Chem Lett       Date:  2010-06-15       Impact factor: 2.823

5.  Chemical lead optimization of a pan Gq mAChR M1, M3, M5 positive allosteric modulator (PAM) lead. Part II: development of a potent and highly selective M1 PAM.

Authors:  Thomas M Bridges; J Phillip Kennedy; Meredith J Noetzel; Micah L Breininger; Patrick R Gentry; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2010-02-01       Impact factor: 2.823

6.  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

7.  Synthesis and SAR of analogs of the M1 allosteric agonist TBPB. Part II: Amides, sulfonamides and ureas--the effect of capping the distal basic piperidine nitrogen.

Authors:  Nicole R Miller; R Nathan Daniels; Thomas M Bridges; Ashley E Brady; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2008-09-11       Impact factor: 2.823

Review 8.  Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Carrie K Jones; Craig W Lindsley
Journal:  Trends Pharmacol Sci       Date:  2009-02-07       Impact factor: 14.819

9.  Discovery of the first highly M5-preferring muscarinic acetylcholine receptor ligand, an M5 positive allosteric modulator derived from a series of 5-trifluoromethoxy N-benzyl isatins.

Authors:  Thomas M Bridges; Joy E Marlo; Colleen M Niswender; Carrie K Jones; Satyawan B Jadhav; Patrick R Gentry; Hyekyung C Plumley; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2009-06-11       Impact factor: 7.446

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
View more
  16 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

Review 2.  Muscarinic and nicotinic acetylcholine receptor agonists and allosteric modulators for the treatment of schizophrenia.

Authors:  Carrie K Jones; Nellie Byun; Michael Bubser
Journal:  Neuropsychopharmacology       Date:  2011-09-28       Impact factor: 7.853

3.  Selective syntheses of no-carrier-added 2- and 3-[18F]fluorohalopyridines through the radiofluorination of halopyridinyl(4'-methoxyphenyl)iodonium tosylates.

Authors:  Joong-Hyun Chun; Victor W Pike
Journal:  Chem Commun (Camb)       Date:  2012-08-30       Impact factor: 6.222

Review 4.  Emerging approaches for treatment of schizophrenia: modulation of cholinergic signaling.

Authors:  Daniel J Foster; Carrie K Jones; P Jeffrey Conn
Journal:  Discov Med       Date:  2012-12       Impact factor: 2.970

5.  Development of novel M1 antagonist scaffolds through the continued optimization of the MLPCN probe ML012.

Authors:  Bruce J Melancon; Thomas J Utley; Christian Sevel; Margrith E Mattmann; Yiu-Yin Cheung; Thomas M Bridges; Ryan D Morrison; Douglas J Sheffler; Colleen M Niswender; J Scott Daniels; P Jeffrey Conn; Craig W Lindsley; Michael R Wood
Journal:  Bioorg Med Chem Lett       Date:  2012-06-15       Impact factor: 2.823

6.  Discovery and optimization of a novel, selective and brain penetrant M1 positive allosteric modulator (PAM): the development of ML169, an MLPCN probe.

Authors:  Paul R Reid; Thomas M Bridges; Douglas J Sheffler; Hyekyung P Cho; L Michelle Lewis; Emily Days; J Scott Daniels; Carrie K Jones; Colleen M Niswender; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Michael R Wood
Journal:  Bioorg Med Chem Lett       Date:  2010-12-09       Impact factor: 2.823

7.  Development of a more highly selective M(1) antagonist from the continued optimization of the MLPCN Probe ML012.

Authors:  Bruce J Melancon; Alexander P Lamers; Thomas M Bridges; Gary A Sulikowski; Thomas J Utley; Douglas J Sheffler; Meredith J Noetzel; Ryan D Morrison; J Scott Daniels; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Michael R Wood
Journal:  Bioorg Med Chem Lett       Date:  2011-12-06       Impact factor: 2.823

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

9.  Structural modifications to tetrahydropyridine-3-carboxylate esters en route to the discovery of M5-preferring muscarinic receptor orthosteric antagonists.

Authors:  Guangrong Zheng; Andrew M Smith; Xiaoqin Huang; Karunai L Subramanian; Kiran B Siripurapu; Agripina Deaciuc; Chang-Guo Zhan; Linda P Dwoskin
Journal:  J Med Chem       Date:  2013-02-18       Impact factor: 7.446

10.  Discovery of ML326: The first sub-micromolar, selective M5 PAM.

Authors:  Patrick R Gentry; Thomas M Bridges; Atin Lamsal; Paige N Vinson; Emery Smith; Peter Chase; Peter S Hodder; Julie L Engers; Colleen M Niswender; J Scott Daniels; P Jeffrey Conn; Michael R Wood; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2013-03-16       Impact factor: 2.823
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.