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Items: 1 to 20 of 109


Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.

Paoletta S, Tosh DK, Finley A, Gizewski ET, Moss SM, Gao ZG, Auchampach JA, Salvemini D, Jacobson KA.

J Med Chem. 2013 Jul 25;56(14):5949-63. doi: 10.1021/jm4007966. Epub 2013 Jul 3.


Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists.

Nayak A, Chandra G, Hwang I, Kim K, Hou X, Kim HO, Sahu PK, Roy KK, Yoo J, Lee Y, Cui M, Choi S, Moss SM, Phan K, Gao ZG, Ha H, Jacobson KA, Jeong LS.

J Med Chem. 2014 Feb 27;57(4):1344-54. doi: 10.1021/jm4015313. Epub 2014 Feb 5.


In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.

Tosh DK, Finley A, Paoletta S, Moss SM, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.

J Med Chem. 2014 Dec 11;57(23):9901-14. doi: 10.1021/jm501021n. Epub 2014 Nov 25.


Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.

Tosh DK, Deflorian F, Phan K, Gao ZG, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.

J Med Chem. 2012 May 24;55(10):4847-60. doi: 10.1021/jm300396n. Epub 2012 May 16.


Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor.

Tosh DK, Paoletta S, Chen Z, Moss SM, Gao ZG, Salvemini D, Jacobson KA.

Bioorg Med Chem Lett. 2014 Aug 1;24(15):3302-6. doi: 10.1016/j.bmcl.2014.06.006. Epub 2014 Jun 11.


Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.

Tosh DK, Chinn M, Ivanov AA, Klutz AM, Gao ZG, Jacobson KA.

J Med Chem. 2009 Dec 10;52(23):7580-92. doi: 10.1021/jm900426g.


Characterization by flow cytometry of fluorescent, selective agonist probes of the A(3) adenosine receptor.

Kozma E, Gizewski ET, Tosh DK, Squarcialupi L, Auchampach JA, Jacobson KA.

Biochem Pharmacol. 2013 Apr 15;85(8):1171-81. doi: 10.1016/j.bcp.2013.01.021. Epub 2013 Jan 31.


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

Tchilibon S, Joshi BV, Kim SK, Duong HT, Gao ZG, Jacobson KA.

J Med Chem. 2005 Mar 24;48(6):1745-58.


Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.

Melman A, Wang B, Joshi BV, Gao ZG, Castro Sd, Heller CL, Kim SK, Jeong LS, Jacobson KA.

Bioorg Med Chem. 2008 Sep 15;16(18):8546-56. doi: 10.1016/j.bmc.2008.08.007. Epub 2008 Aug 7.


Synthesis and evaluation of N⁶-substituted apioadenosines as potential adenosine A₃ receptor modulators.

Toti KS, Moss SM, Paoletta S, Gao ZG, Jacobson KA, Van Calenbergh S.

Bioorg Med Chem. 2014 Aug 1;22(15):4257-68. doi: 10.1016/j.bmc.2014.05.036. Epub 2014 May 23.


Probing the binding site of the A1 adenosine receptor reengineered for orthogonal recognition by tailored nucleosides.

Palaniappan KK, Gao ZG, Ivanov AA, Greaves R, Adachi H, Besada P, Kim HO, Kim AY, Choe SA, Jeong LS, Jacobson KA.

Biochemistry. 2007 Jun 26;46(25):7437-48. Epub 2007 Jun 2.


2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists.

Tosh DK, Chinn M, Yoo LS, Kang DW, Luecke H, Gao ZG, Jacobson KA.

Bioorg Med Chem. 2010 Jan 15;18(2):508-17. doi: 10.1016/j.bmc.2009.12.018. Epub 2009 Dec 11.


Structure-Based Design, Synthesis by Click Chemistry and in Vivo Activity of Highly Selective A3 Adenosine Receptor Agonists.

Tosh DK, Paoletta S, Chen Z, Crane S, Lloyd J, Gao ZG, Gizewski ET, Auchampach JA, Salvemini D, Jacobson KA.

Medchemcomm. 2015;6:555-563.


Discovery of simplified N²-substituted pyrazolo[3,4-d]pyrimidine derivatives as novel adenosine receptor antagonists: efficient synthetic approaches, biological evaluations and molecular docking studies.

Venkatesan G, Paira P, Cheong SL, Vamsikrishna K, Federico S, Klotz KN, Spalluto G, Pastorin G.

Bioorg Med Chem. 2014 Mar 1;22(5):1751-65. doi: 10.1016/j.bmc.2014.01.018. Epub 2014 Jan 31.


Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.

Li AH, Moro S, Forsyth N, Melman N, Ji XD, Jacobson KA.

J Med Chem. 1999 Feb 25;42(4):706-21.


Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.

Melman A, Gao ZG, Kumar D, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.

Bioorg Med Chem Lett. 2008 May 1;18(9):2813-9. doi: 10.1016/j.bmcl.2008.04.001. Epub 2008 Apr 4.


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

Tosh DK, Paoletta S, Deflorian F, Phan K, Moss SM, Gao ZG, Jiang X, Jacobson KA.

J Med Chem. 2012 Sep 27;55(18):8075-90. Epub 2012 Sep 10.


Click modification in the N6 region of A3 adenosine receptor-selective carbocyclic nucleosides for dendrimeric tethering that preserves pharmacophore recognition.

Tosh DK, Phan K, Deflorian F, Wei Q, Yoo LS, Gao ZG, Jacobson KA.

Bioconjug Chem. 2012 Feb 15;23(2):232-47. doi: 10.1021/bc200526c. Epub 2012 Jan 11.


Purine derivatives as ligands for A3 adenosine receptors.

Joshi BV, Jacobson KA.

Curr Top Med Chem. 2005;5(13):1275-95. Review.

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