Literature DB >> 17045477

N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists.

Elfatih Elzein1, Rao Kalla, Xiaofen Li, Thao Perry, Tim Marquart, Mark Micklatcher, Yuan Li, Yuzhi Wu, Dewan Zeng, Jeff Zablocki.   

Abstract

A series of new selective, high affinity A(1)-AdoR agonists is reported. Compound 23 that incorporated a carboxylic acid functionality in the 4-position of the pyrazole ring displayed K(iL) value of 1 nM for the A(1)-AdoR and >5000-fold selectivity over the A(3) and A(2A)-AdoRs. In addition, compound 19 that incorporated a carboxamide functionality in the 4-position of the pyrazole ring displayed subnanomolar affinity for the A(1)-AdoR (K(iL)=0.6 nM) and >600-fold selectivity over the A(3) and A(2A)-AdoRs.

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Year:  2006        PMID： 17045477     DOI： 10.1016/j.bmcl.2006.09.065

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


  6 in total

1.  Synthesis of purine modified 2'-C-methyl nucleosides as potential anti-HCV agents.

Authors:  Hong-wang Zhang; Longhu Zhou; Steven J Coats; Tamara R McBrayer; Phillip M Tharnish; Lavanya Bondada; Mervi Detorio; Sarah A Amichai; Melissa D Johns; Tony Whitaker; Raymond F Schinazi
Journal:  Bioorg Med Chem Lett       Date:  2011-09-20       Impact factor: 2.823

2.  A3 adenosine receptor agonists containing dopamine moieties for enhanced interspecies affinity.

Authors:  Dilip K Tosh; Veronica Salmaso; Ryan G Campbell; Harsha Rao; Amelia Bitant; Eline Pottie; Christophe P Stove; Naili Liu; Oksana Gavrilova; Zhan-Guo Gao; John A Auchampach; Kenneth A Jacobson
Journal:  Eur J Med Chem       Date:  2021-11-19       Impact factor: 6.514

3.  Design and in Vivo Characterization of A1 Adenosine Receptor Agonists in the Native Ribose and Conformationally Constrained (N)-Methanocarba Series.

Authors:  Dilip K Tosh; Harsha Rao; Amelia Bitant; Veronica Salmaso; Philip Mannes; David I Lieberman; Kelli L Vaughan; Julie A Mattison; Amy C Rothwell; John A Auchampach; Antonella Ciancetta; Naili Liu; Zhenzhong Cui; Zhan-Guo Gao; Marc L Reitman; Oksana Gavrilova; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2019-01-03       Impact factor: 7.446

4.  Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.

Authors:  Dilip K Tosh; Silvia Paoletta; Francesca Deflorian; Khai Phan; Steven M Moss; Zhan-Guo Gao; Xiaohui Jiang; Kenneth A Jacobson
Journal:  J Med Chem       Date:  2012-09-10       Impact factor: 7.446

5.  Synthesis and Evaluation of 2,6-Modified Purine 2'-C-Methyl Ribonucleosides as Inhibitors of HCV Replication.

Authors:  Longhu Zhou; Hongwang Zhang; Sijia Tao; Maryam Ehteshami; Jong Hyun Cho; Tamara R McBrayer; Philip Tharnish; Tony Whitaker; Franck Amblard; Steven J Coats; Raymond F Schinazi
Journal:  ACS Med Chem Lett       Date:  2015-11-23       Impact factor: 4.345

6.  1,2,3-Triazoles as leaving groups: SNAr reactions of 2,6-bistriazolylpurines with O- and C-nucleophiles.

Authors:  Dace Cīrule; Irina Novosjolova; Ērika Bizdēna; Māris Turks
Journal:  Beilstein J Org Chem       Date:  2021-02-11       Impact factor: 2.883
  6 in total

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