Literature DB >> 12039562

2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors.

Mahendra D Chordia1, Lauren J Murphree, Timothy L Macdonald, Joel Linden, Ray A Olsson.   

Abstract

This report describes the synthesis and structure-activity relationships of a new class of A(1) adenosine receptor agonist allosteric enhancers, 2-aminothiazolium salts. The EC(50) of compounds 6a, 6b, 7, and 8 were 0.3, 4.5, 3.8, and 1.2 microM, substantially lower than that of the 'Gold Standard' 2-amino-3-benzoyl thiophene (PD 81,723), which has an EC(50) of 38 microM.

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Year:  2002        PMID： 12039562     DOI： 10.1016/s0960-894x(02)00236-6

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


  8 in total

1.  Identification of potent tricyclic prodrug S1P1 receptor modulators.

Authors:  David Marcoux; Hai-Yun Xiao; T G Murali Dhar; Jenny Xie; Lois D Lehman-McKeeman; Dauh-Rurng Wu; Marta Dabros; Xiaoxia Yang; Tracy L Taylor; Xia D Zhou; Elizabeth M Heimrich; Rochelle Thomas; Kim W McIntyre; Hong Shi; Paul C Levesque; Huadong Sun; Zheng Yang; Anthony M Marino; Georgia Cornelius; Celia J D'Arienzo; Anuradha Gupta; Bala Pragalathan; Richard Rampulla; Arvind Mathur; Ding Ren Shen; Mary Ellen Cvijic; Luisa Salter-Cid; Louis J Lombardo; Percy H Carter; Alaric J Dyckman
Journal:  Medchemcomm       Date:  2016-11-25       Impact factor: 3.597

2.  A Facile Approach to the Synthesis of 3,4-Disubstituted-2-Aminothiazolium Derivatives through the Use of A "Volatilizable" Support.

Authors:  Yangmei Li; Marc Giulianotti; Richard A Houghten
Journal:  Tetrahedron Lett       Date:  2010-10-27       Impact factor: 2.415

3.  Analogs of N'-hydroxy-N-(4H,5H-naphtho[1,2-d]thiazol-2-yl)methanimidamide inhibit Mycobacterium tuberculosis methionine aminopeptidases.

Authors:  Shridhar Bhat; Omonike Olaleye; Kirsten J Meyer; Wanliang Shi; Ying Zhang; Jun O Liu
Journal:  Bioorg Med Chem       Date:  2012-05-17       Impact factor: 3.641

4.  Synthesis and Biochemical Evaluation of 8H-Indeno[1,2-d]thiazole Derivatives as Novel SARS-CoV-2 3CL Protease Inhibitors.

Authors:  Jing Wu; Bo Feng; Li-Xin Gao; Chun Zhang; Jia Li; Da-Jun Xiang; Yi Zang; Wen-Long Wang
Journal:  Molecules       Date:  2022-05-23       Impact factor: 4.927

5.  2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.

Authors:  Gemma N Ferguson; Celine Valant; James Horne; Heidi Figler; Bernard L Flynn; Joel Linden; David K Chalmers; Patrick M Sexton; Arthur Christopoulos; Peter J Scammells
Journal:  J Med Chem       Date:  2008-09-05       Impact factor: 7.446

Review 6.  Allosteric modulation of the adenosine family of receptors.

Authors:  Zhan-Guo Gao; Soo-Kyung Kim; Adriaan P Ijzerman; Kenneth A Jacobson
Journal:  Mini Rev Med Chem       Date:  2005-06       Impact factor: 3.862

7.  Allosteric modulation of adenosine receptors.

Authors:  Anikó Göblyös; Ad P Ijzerman
Journal:  Purinergic Signal       Date:  2008-07-10       Impact factor: 3.765

8.  Synthesis of rigidified eIF4E/eIF4G inhibitor-1 (4EGI-1) mimetic and their in vitro characterization as inhibitors of protein-protein interaction.

Authors:  Poornachandran Mahalingam; Khuloud Takrouri; Ting Chen; Rupam Sahoo; Evangelos Papadopoulos; Limo Chen; Gerhard Wagner; Bertal H Aktas; Jose A Halperin; Michael Chorev
Journal:  J Med Chem       Date:  2014-06-04       Impact factor: 7.446
  8 in total

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