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Studies on enantioselectivity of chiral 4-acetylamino-6-alkyloxy-2-alkylthiopyrimidines acting as antagonists of the human A3 adenosine receptor.

Cosimelli B, Greco G, Laneri S, Novellino E, Sacchi A, Collina S, Rossi D, Cosconati S, Barresi E, Taliani S, Trincavelli ML, Martini C.

Medchemcomm. 2017 Nov 9;9(1):81-86. doi: 10.1039/c7md00375g. eCollection 2018 Jan 1.


Enantiomeric 4-Acylamino-6-alkyloxy-2 Alkylthiopyrimidines As Potential A3 Adenosine Receptor Antagonists: HPLC Chiral Resolution and Absolute Configuration Assignment by a Full Set of Chiroptical Spectroscopy.

Rossi D, Nasti R, Marra A, Meneghini S, Mazzeo G, Longhi G, Memo M, Cosimelli B, Greco G, Novellino E, Da Settimo F, Martini C, Taliani S, Abbate S, Collina S.

Chirality. 2016 May;28(5):434-40. doi: 10.1002/chir.22599. Epub 2016 Apr 20.


Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.

Kim YC, de Zwart M, Chang L, Moro S, von Frijtag Drabbe Künzel JK, Melman N, IJzerman AP, Jacobson KA.

J Med Chem. 1998 Jul 16;41(15):2835-45.


5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.

Da Settimo F, Primofiore G, Taliani S, Marini AM, La Motta C, Simorini F, Salerno S, Sergianni V, Tuccinardi T, Martinelli A, Cosimelli B, Greco G, Novellino E, Ciampi O, Trincavelli ML, Martini C.

J Med Chem. 2007 Nov 15;50(23):5676-84. Epub 2007 Oct 10.


Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors.

Alnouri MW, Jepards S, Casari A, Schiedel AC, Hinz S, Müller CE.

Purinergic Signal. 2015 Sep;11(3):389-407. doi: 10.1007/s11302-015-9460-9. Epub 2015 Jul 1.


Insight into the interactions between novel coumarin derivatives and human A3 adenosine receptors.

Matos MJ, Vilar S, Kachler S, Fonseca A, Santana L, Uriarte E, Borges F, Tatonetti NP, Klotz KN.

ChemMedChem. 2014 Oct;9(10):2245-53. doi: 10.1002/cmdc.201402205. Epub 2014 Jul 18.


A1 adenosine receptor negatively modulates coronary reactive hyperemia via counteracting A2A-mediated H2O2 production and KATP opening in isolated mouse hearts.

Zhou X, Teng B, Tilley S, Mustafa SJ.

Am J Physiol Heart Circ Physiol. 2013 Dec 1;305(11):H1668-79. doi: 10.1152/ajpheart.00495.2013. Epub 2013 Sep 16.


Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.

Baraldi PG, Cacciari B, Pineda de Las Infantas MJ, Romagnoli R, Spalluto G, Volpini R, Costanzi S, Vittori S, Cristalli G, Melman N, Park KS, Ji XD, Jacobson KA.

J Med Chem. 1998 Aug 13;41(17):3174-85.


4-amino-6-alkyloxy-2-alkylthiopyrimidine derivatives as novel non-nucleoside agonists for the adenosine A1 receptor.

Cosimelli B, Greco G, Laneri S, Novellino E, Sacchi A, Trincavelli ML, Giacomelli C, Taliani S, Da Settimo F, Martini C.

Chem Biol Drug Des. 2016 Nov;88(5):724-729. doi: 10.1111/cbdd.12801. Epub 2016 Jul 11.


Novel human adenosine receptor antagonists based on the 7-amino-thiazolo[5,4-d]pyrimidine scaffold. Structural investigations at the 2-, 5- and 7-positions to enhance affinity and tune selectivity.

Varano F, Catarzi D, Falsini M, Dal Ben D, Buccioni M, Marucci G, Volpini R, Colotta V.

Bioorg Med Chem Lett. 2019 Feb 15;29(4):563-569. doi: 10.1016/j.bmcl.2018.12.062. Epub 2018 Dec 31.


Allosteric modulators of human A2B adenosine receptor.

Trincavelli ML, Giacomelli C, Daniele S, Taliani S, Cosimelli B, Laneri S, Severi E, Barresi E, Pugliesi I, Greco G, Novellino E, Da Settimo F, Martini C.

Biochim Biophys Acta. 2014 Mar;1840(3):1194-203. doi: 10.1016/j.bbagen.2013.12.021. Epub 2013 Dec 19.


Probing Substituents in the 1- and 3-Position: Tetrahydropyrazino-Annelated Water-Soluble Xanthine Derivatives as Multi-Target Drugs With Potent Adenosine Receptor Antagonistic Activity.

Koch P, Brunschweiger A, Namasivayam V, Ullrich S, Maruca A, Lazzaretto B, Küppers P, Hinz S, Hockemeyer J, Wiese M, Heer J, Alcaro S, Kiec-Kononowicz K, Müller CE.

Front Chem. 2018 Jun 26;6:206. doi: 10.3389/fchem.2018.00206. eCollection 2018.


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.


2-Amino[1,2,4]triazolo[1,5-c]quinazolines and Derived Novel Heterocycles: Syntheses and Structure-Activity Relationships of Potent Adenosine Receptor Antagonists.

Burbiel JC, Ghattas W, Küppers P, Köse M, Lacher S, Herzner AM, Kombu RS, Akkinepally RR, Hockemeyer J, Müller CE.

ChemMedChem. 2016 Oct 19;11(20):2272-2286. doi: 10.1002/cmdc.201600255. Epub 2016 Aug 17.


Exploring the 7-oxo-thiazolo[5,4-d]pyrimidine core for the design of new human adenosine A3 receptor antagonists. Synthesis, molecular modeling studies and pharmacological evaluation.

Varano F, Catarzi D, Squarcialupi L, Betti M, Vincenzi F, Ravani A, Varani K, Dal Ben D, Thomas A, Volpini R, Colotta V.

Eur J Med Chem. 2015;96:105-21. doi: 10.1016/j.ejmech.2015.04.010. Epub 2015 Apr 4.


Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.

Baraldi PG, Tabrizi MA, Preti D, Bovero A, Romagnoli R, Fruttarolo F, Zaid NA, Moorman AR, Varani K, Gessi S, Merighi S, Borea PA.

J Med Chem. 2004 Mar 11;47(6):1434-47.


N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.

Volpini R, Dal Ben D, Lambertucci C, Taffi S, Vittori S, Klotz KN, Cristalli G.

J Med Chem. 2007 Mar 22;50(6):1222-30. Epub 2007 Feb 20.


The Influence of the 1-(3-Trifluoromethyl-Benzyl)-1H-Pyrazole-4-yl Moiety on the Adenosine Receptors Affinity Profile of Pyrazolo[4,3-e][1,2,4]Triazolo[1,5-c]Pyrimidine Derivatives.

Federico S, Redenti S, Sturlese M, Ciancetta A, Kachler S, Klotz KN, Cacciari B, Moro S, Spalluto G.

PLoS One. 2015 Dec 1;10(12):e0143504. doi: 10.1371/journal.pone.0143504. eCollection 2015.


Antiproliferative effects of selective adenosine receptor agonists and antagonists on human lymphocytes: evidence for receptor-independent mechanisms.

Schiedel AC, Lacher SK, Linnemann C, Knolle PA, Müller CE.

Purinergic Signal. 2013 Sep;9(3):351-65. doi: 10.1007/s11302-013-9354-7. Epub 2013 Jan 29.

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