Literature DB >> 12657269

Novel and potent human and rat beta3-adrenergic receptor agonists containing substituted 3-indolylalkylamines.

Hiroshi Harada1, Yoshimi Hirokawa, Kenji Suzuki, Yoichi Hiyama, Mayumi Oue, Hitoshi Kawashima, Naoyuki Yoshida, Yasuji Furutani, Shiro Kato.   

Abstract

A novel series of 2-(3-indolyl)alkylamino-1-(3-chlorophenyl)ethanols was prepared and evaluated for in vitro ability to stimulate cAMP production in Chinese hamster ovary cells expressing cloned human beta(3)-AR. The optically active 30a was found to be the most potent and selective human beta(3)-AR agonist in this series with an EC(50) value of 0.062nM. In addition, 30a selectivity for human beta(3)-AR was 210-fold and 103-fold that for human beta(2)-AR and beta(1)-AR, respectively. Furthermore, 30a showed potent agonistic activity at rat beta(3)-AR.

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Year:  2003        PMID： 12657269     DOI： 10.1016/s0960-894x(03)00073-8

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


  5 in total

1.  Structural characterization and computer-aided optimization of a small-molecule inhibitor of the Arp2/3 complex, a key regulator of the actin cytoskeleton.

Authors:  Andrew W Baggett; Zoe Cournia; Min Suk Han; George Patargias; Adam C Glass; Shih-Yuan Liu; Brad J Nolen
Journal:  ChemMedChem       Date:  2012-05-23       Impact factor: 3.466

2.  Comparative 3D QSAR study on β(1)-, β(2)-, and β(3)-adrenoceptor agonists.

Authors:  P Senthil Kumar; Prasad V Bharatam
Journal:  Med Chem Res       Date:  2009-10-31       Impact factor: 1.965

3.  2D-QSAR and 3D-QSAR/CoMSIA Studies on a Series of (R)-2-((2-(1H-Indol-2-yl)ethyl)amino)-1-Phenylethan-1-ol with Human β₃-Adrenergic Activity.

Authors:  Gastón Apablaza; Luisa Montoya; Cesar Morales-Verdejo; Marco Mellado; Mauricio Cuellar; Carlos F Lagos; Jorge Soto-Delgado; Hery Chung; Carlos David Pessoa-Mahana; Jaime Mella
Journal:  Molecules       Date:  2017-03-05       Impact factor: 4.411

4.  Spirotetrahydro beta-carbolines (spiroindolones): a new class of potent and orally efficacious compounds for the treatment of malaria.

Authors:  Bryan K S Yeung; Bin Zou; Matthias Rottmann; Suresh B Lakshminarayana; Shi Hua Ang; Seh Yong Leong; Jocelyn Tan; Josephine Wong; Sonja Keller-Maerki; Christoph Fischli; Anne Goh; Esther K Schmitt; Philipp Krastel; Eric Francotte; Kelli Kuhen; David Plouffe; Kerstin Henson; Trixie Wagner; Elizabeth A Winzeler; Frank Petersen; Reto Brun; Veronique Dartois; Thierry T Diagana; Thomas H Keller
Journal:  J Med Chem       Date:  2010-07-22       Impact factor: 7.446

5.  Pharmacophore-guided Virtual Screening to Identify New β3 -adrenergic Receptor Agonists.

Authors:  Navista Sri Octa Ujiantari; Seungmin Ham; Chisae Nagiri; Wataru Shihoya; Osamu Nureki; Dana Sabine Hutchinson; Daniela Schuster
Journal:  Mol Inform       Date:  2022-02-02       Impact factor: 4.050
  5 in total

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