Literature DB >> 20483599

2' biaryl amides as novel and subtype selective M1 agonists. Part II: Further optimization and profiling.

Brian Budzik1, Vincenzo Garzya, Dongchuan Shi, Graham Walker, Yann Lauchart, Adam J Lucas, Ralph A Rivero, Christopher J Langmead, Jeannette Watson, Zining Wu, Ian T Forbes, Jian Jin.   

Abstract

Further optimization of the biaryl amide series via extensively exploring structure-activity relationships resulted in potent and subtype selective M(1) agonists exemplified by compounds 9a and 9j with good rat PK properties including CNS penetration. Synthesis, structure-activity relationships, subtype selectivity for M(1) over M(2-5), and DMPK properties of these novel compounds are described. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20483599     DOI： 10.1016/j.bmcl.2010.04.127

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


  6 in total

Review 1.  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

2.  Novel N-Substituted Benzimidazolones as Potent, Selective, CNS-Penetrant, and Orally Active M1 mAChR Agonists.

Authors:  Brian Budzik; Vincenzo Garzya; Dongchuan Shi; Graham Walker; Marie Woolley-Roberts; Joanne Pardoe; Adam Lucas; Ben Tehan; Ralph A Rivero; Christopher J Langmead; Jeannette Watson; Zining Wu; Ian T Forbes; Jian Jin
Journal:  ACS Med Chem Lett       Date:  2010-06-08       Impact factor: 4.345

Review 3.  Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.

Authors:  Bruce J Melancon; James C Tarr; Joseph D Panarese; Michael R Wood; Craig W Lindsley
Journal:  Drug Discov Today       Date:  2013-09-17       Impact factor: 7.851

4.  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

Review 5.  Progress in structure based drug design for G protein-coupled receptors.

Authors:  Miles Congreve; Christopher J Langmead; Jonathan S Mason; Fiona H Marshall
Journal:  J Med Chem       Date:  2011-06-15       Impact factor: 7.446

Review 6.  Potential Role for Combined Subtype-Selective Targeting of M1 and M3 Muscarinic Receptors in Gastrointestinal and Liver Diseases.

Authors:  Mazen Tolaymat; Margaret H Sundel; Madeline Alizadeh; Guofeng Xie; Jean-Pierre Raufman
Journal:  Front Pharmacol       Date:  2021-11-04       Impact factor: 5.810
  6 in total

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