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Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process.
Pastorin G, Federico S, Paoletta S, Corradino M, Cateni F, Cacciari B, Klotz KN, Gao ZG, Jacobson KA, Spalluto G, Moro S. Pastorin G, et al. Among authors: cacciari b. Bioorg Med Chem. 2010 Apr 1;18(7):2524-36. doi: 10.1016/j.bmc.2010.02.039. Epub 2010 Feb 25. Bioorg Med Chem. 2010. PMID: 20304654 Free PMC article.
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as adenosine receptor antagonists. Influence of the N5 substituent on the affinity at the human A 3 and A 2B adenosine receptor subtypes: a molecular modeling investigation.
Pastorin G, Da Ros T, Spalluto G, Deflorian F, Moro S, Cacciari B, Baraldi PG, Gessi S, Varani K, Borea PA. Pastorin G, et al. Among authors: cacciari b. J Med Chem. 2003 Sep 25;46(20):4287-96. doi: 10.1021/jm030852k. J Med Chem. 2003. PMID: 13678407
Combined target-based and ligand-based drug design approach as a tool to define a novel 3D-pharmacophore model of human A3 adenosine receptor antagonists: pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as a key study.
Moro S, Braiuca P, Deflorian F, Ferrari C, Pastorin G, Cacciari B, Baraldi PG, Varani K, Borea PA, Spalluto G. Moro S, et al. Among authors: cacciari b. J Med Chem. 2005 Jan 13;48(1):152-62. doi: 10.1021/jm049662f. J Med Chem. 2005. PMID: 15634009
Synthesis and biological studies of a new series of 5-heteroarylcarbamoylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists. Influence of the heteroaryl substituent on binding affinity and molecular modeling investigations.
Pastorin G, Da Ros T, Bolcato C, Montopoli C, Moro S, Cacciari B, Baraldi PG, Varani K, Borea PA, Spalluto G. Pastorin G, et al. Among authors: cacciari b. J Med Chem. 2006 Mar 9;49(5):1720-9. doi: 10.1021/jm051147+. J Med Chem. 2006. PMID: 16509587
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.
Michielan L, Bolcato C, Federico S, Cacciari B, Bacilieri M, Klotz KN, Kachler S, Pastorin G, Cardin R, Sperduti A, Spalluto G, Moro S. Michielan L, et al. Among authors: cacciari b. Bioorg Med Chem. 2009 Jul 15;17(14):5259-74. doi: 10.1016/j.bmc.2009.05.038. Epub 2009 May 21. Bioorg Med Chem. 2009. PMID: 19501513
The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA(3) adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognition.
Cheong SL, Dolzhenko A, Kachler S, Paoletta S, Federico S, Cacciari B, Dolzhenko A, Klotz KN, Moro S, Spalluto G, Pastorin G. Cheong SL, et al. Among authors: cacciari b. J Med Chem. 2010 Apr 22;53(8):3361-75. doi: 10.1021/jm100049f. J Med Chem. 2010. PMID: 20307065
Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility.
Federico S, Paoletta S, Cheong SL, Pastorin G, Cacciari B, Stragliotto S, Klotz KN, Siegel J, Gao ZG, Jacobson KA, Moro S, Spalluto G. Federico S, et al. Among authors: cacciari b. J Med Chem. 2011 Feb 10;54(3):877-89. doi: 10.1021/jm101349u. Epub 2011 Jan 7. J Med Chem. 2011. PMID: 21214204 Free PMC article.
Exploring the directionality of 5-substitutions in a new series of 5-alkylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine as a strategy to design novel human a(3) adenosine receptor antagonists.
Federico S, Ciancetta A, Sabbadin D, Paoletta S, Pastorin G, Cacciari B, Klotz KN, Moro S, Spalluto G. Federico S, et al. Among authors: cacciari b. J Med Chem. 2012 Nov 26;55(22):9654-68. doi: 10.1021/jm300899q. Epub 2012 Nov 9. J Med Chem. 2012. PMID: 23098605
79 results