Literature DB >> 9873431

The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.

J P Mogensen1, S M Roberts, A N Bowler, C Thomsen, L J Knutsen.   

Abstract

The synthesis and purinergic receptor binding of novel adenosine A3 ligands is described. Many selective A3 receptor agonists e.g. N-(3-iodobenzyl)adenosine-5'-methyluronamide (IB-MECA) contain a 4'-ribosylalkylamide moiety. We found that this amide and other 4'-functional groups could be replaced with an isosteric isoxazole, and the target molecules retained potent binding to the recombinant human A3 receptor.

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Year:  1998        PMID： 9873431     DOI： 10.1016/s0960-894x(98)00302-3

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


  8 in total

1.  Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.

Authors:  K Lee; G Ravi; X D Ji; V E Marquez; K A Jacobson
Journal:  Bioorg Med Chem Lett       Date:  2001-05-21       Impact factor: 2.823

2.  Chapter 13. A3 Adenosine Receptors.

Authors:  Kenneth A Jacobson; Susanna Tchilibon; Bhalchandra V Joshi; Zhan-Guo Gao
Journal:  Annu Rep Med Chem       Date:  2003       Impact factor: 1.059

3.  (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.

Authors:  Susanna Tchilibon; Bhalchandra V Joshi; Soo-Kyung Kim; Heng T Duong; Zhan-Guo Gao; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2005-03-24       Impact factor: 7.446

Review 4.  A3 Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy.

Authors:  Kenneth A Jacobson; Stefania Merighi; Katia Varani; Pier Andrea Borea; Stefania Baraldi; Mojgan Aghazadeh Tabrizi; Romeo Romagnoli; Pier Giovanni Baraldi; Antonella Ciancetta; Dilip K Tosh; Zhan-Guo Gao; Stefania Gessi
Journal:  Med Res Rev       Date:  2017-07-06       Impact factor: 12.944

5.  "Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.

Authors:  Melissa Perreira; Jian-Kang Jiang; Athena M Klutz; Zhan-Guo Gao; Asher Shainberg; Changrui Lu; Craig J Thomas; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2005-07-28       Impact factor: 7.446

6.  Modulation of adenosine receptor affinity and intrinsic efficacy in adenine nucleosides substituted at the 2-position.

Authors:  Michihiro Ohno; Zhan-Guo Gao; Philippe Van Rompaey; Susanna Tchilibon; Soo-Kyung Kim; Brian A Harris; Ariel S Gross; Heng T Duong; Serge Van Calenbergh; Kenneth A Jacobson
Journal:  Bioorg Med Chem       Date:  2004-06-01       Impact factor: 3.641

7.  N6-Substituted adenosine derivatives: selectivity, efficacy, and species differences at A3 adenosine receptors.

Authors:  Zhan-Guo Gao; Joshua B Blaustein; Ariel S Gross; Neli Melman; Kenneth A Jacobson
Journal:  Biochem Pharmacol       Date:  2003-05-15       Impact factor: 5.858

Review 8.  Partial agonists for A(3) adenosine receptors.

Authors:  Zhan-Guo Gao; Kenneth A Jacobson
Journal:  Curr Top Med Chem       Date:  2004       Impact factor: 3.295
  8 in total

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