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14998332,18077171,16759111,22148859,16275090,15788741,16219300,16392813,19398343,18938084,13678407,18226909,16033279,15771453,21675777,14761205,20137957,19682912,19639280,15177484,16186657,18226896,18000937,19569717,20307065,20371139,15267242,16847822,19346133,18321039,15464622,16250647,16821798,16000006,10737749,16386423,10496952,16697192,19036477,12646033,15961085,17300165,22409573,15748700,17306548,11906291,17469811,15214785,12593659,17382926,8676354,15341491,18269230,15664822,17228880,15743197,19282184,12672250,22257095,12139454,15689168,9622554,10779381,12014951,19743865,11123985,20937560,19317449,20137946,15481989,20408530,16279775,18407496,18338422,9767637,21908194,18035350,18637670,19301821,23215685,15507216,9435909,16010360,17126322,16509587,23892098,17933541,11266650,10215699,17125264,15476669,17927167,11831890,21664729,3561384,9767636,17827019,11226132,17684118,21766450,16837560,25063944,22568637,24361612,15239649,9191953,23600387,21390354,10212124,24139167,15658856,20541935,14667213,16844379,10639752,10411482,15194002,15588088,8691445,27404511,18979526,22204739,8863798,23266380,18404460,9205770,12570760,20422944,21796795,10669571,12502365,12109910,26625265,10215700,23098605,28415011,9703464,12517430,9681137,23245803,8863792,10212125,7741774,24556147,21186795,18066802,20385496,14640554,10411472,20095134,21401121,9632369,19184536,18443746,23286920,12519065,16902942,12593651,9513594,20018509,11990083,18468446,12139445,23171656,10395488,21764185,27842891,20096593,27836398,10624567,14736246,9933143,26392370,20599769,10052977,25462223,21539392,21388809,32100461,19733067,22292533,12750024,14695840,24118065,20304654,11754583,16581066,11705449,20303771,8258823,21620804,8930114,28114825,14691055,11150167,9767643,8809159,20008542,9371242,20340125,12877594,26126429,14736255,15132536,20455563,12723960,23500543,24077183,27658798,21517076,16366607,8071944,30933785,9888842,14695830,12750027,21036609,11262085,12502367,24332652,12502366,10354408,17077318,24090420,24518296,17499511,22107017,9629466,23631427,11101355,16033270,10411491,19375920,17391106,30108984,32629282,7838877,25874336,11310591,23543220,29681156,26482925,9703463,14584940,9240350,12593665,16243321,12570758,23685887,12369946,8496902,21949117,12712501,12739938,23427825,12822179,7932565,16458010,28217962,17125265,9040991,16289820,27161878,26851736,20034788,20483600,1548682,29998095,11170626,14635095,10841801,11852532,24817533,19908874,20689344,10377236,11809871,8182711,21080722,17149867,30415894,28881253,2754711,21628909,12734636,21802308,12570757,11784146,12620078,25699637,20031412,28789895,22784008,14987833,27150034,9264243,25780876,23789814,11495585,30835463,12878146,21421318,20370659,32962622,14581713,20399651,14642595,29106905,30913470,15743465,9240352,12754103,19772294,9703462,24633424,12801225,21715067,30985956,14640550,32631506,20457527,21377769,21616671,20031406,17168717,21683484,14563788,22182575,20943397,22142423,10514293,18568423,29880250,19846298,21392858,22548457,12502370,20943290,20860381,12930153,21783359,31818481,7766282,20537438,8104517,19896386,11093773,21214204,10411489,22971011,27485602,23231967,12723949,14987824,11557358,12713828,20809633,21055932,32162782,10956189,20652178,21333408,12951147,12723943,12408713,10323559,12540233,33548636,25497490,20347304,27520486,12822180,21473625,17168726,23496127,8064798,12825944,8709114,24677663,12825954,23307426,35790094,17689079,11515591,22433284,3574493,2795597,13678406,22703703,14599553,29353730,14759727,22074142,12491799,7542477,8831777,9089329,20189693,20673729,22559880,9171877,22402302,12467710,32349128,25896847,27718474,12598421,22504568,12166930,31306001,22677030,27721150,22432713,15351792,12063073,15482953,22860174,24161891,19800793,30616250,12852764,27037522,9691247,7487422,25951302,20806896,17378544,19141710,19921682,29525433,25384088,11814828,25044491,8809164,22746350,9484505,3346878,8080613,21277198,21568291,12362366,12762762,35395239,23911855,8230124,19836950,24992070,18404502,20385498,6300892,14640558,21134357,9207941,8080619,32860362,3200248,14695824,18752961,14978249,28344125,20188574,21254595,10090792,24189496,10450966,2709373,20951036,21713967,14584942,14714858,25075638,14760626,17375905,20338760,7727682,12519068,3016270,8043168,8496906,17542617,23342198,22684887,9622556,20105183,31255928,10737748,14981662,22400713,28712806,12729659,10956220,11960496,26160364,19917269,25577710,20144866,21989734,12723950,15615543,12372528,19891474,20579878,20349953,27282729,14565284,1495019,15104242,14697779,31652622,10841798,20121113,12175708,35744918,18776543,9857085,11405649,21945914,19815412,8558508,34120444,11520208,20932745,21353540,3005794,22019467,19589624,10072675,20438717,15070776,2016719,20086038,33316692,8809163,13678411,1501234,22884989,24815000,30638876,12036368,30175951,23953686,20219372,27182099,8872454,22889387,33401004,14711299,2002461,3806597,26824742,34878728,20027670,11714602,18537675,19864133,25982493,17978889,7945524,27721147,26781932,26585572,24252546,31446240,21423433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967 results

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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. Baraldi PG, et al. J Med Chem. 2004 Mar 11;47(6):1434-47. doi: 10.1021/jm0309654. J Med Chem. 2004. PMID: 14998332

1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.

Tabrizi MA, Baraldi PG, Preti D, Romagnoli R, Saponaro G, Baraldi S, Moorman AR, Zaid AN, Varani K, Borea PA. Tabrizi MA, et al. Bioorg Med Chem. 2008 Mar 1;16(5):2419-30. doi: 10.1016/j.bmc.2007.11.058. Epub 2007 Nov 28. Bioorg Med Chem. 2008. PMID: 18077171

Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.

Kalla RV, Elzein E, Perry T, Li X, Palle V, Varkhedkar V, Gimbel A, Maa T, Zeng D, Zablocki J. Kalla RV, et al. J Med Chem. 2006 Jun 15;49(12):3682-92. doi: 10.1021/jm051268+. J Med Chem. 2006. PMID: 16759111

Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A₂B adenosine receptor antagonists.

Baraldi PG, Baraldi S, Saponaro G, Preti D, Romagnoli R, Piccagli L, Cavalli A, Recanatini M, Moorman AR, Zaid AN, Varani K, Borea PA, Tabrizi MA. Baraldi PG, et al. J Med Chem. 2012 Jan 26;55(2):797-811. doi: 10.1021/jm201292w. Epub 2012 Jan 11. J Med Chem. 2012. PMID: 22148859

Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists.

Elzein E, Kalla R, Li X, Perry T, Parkhill E, Palle V, Varkhedkar V, Gimbel A, Zeng D, Lustig D, Leung K, Zablocki J. Elzein E, et al. Bioorg Med Chem Lett. 2006 Jan 15;16(2):302-6. doi: 10.1016/j.bmcl.2005.10.002. Epub 2005 Nov 4. Bioorg Med Chem Lett. 2006. PMID: 16275090

Expression, pharmacological profile, and functional coupling of A2B receptors in a recombinant system and in peripheral blood cells using a novel selective antagonist radioligand, [3H]MRE 2029-F20.

Gessi S, Varani K, Merighi S, Cattabriga E, Pancaldi C, Szabadkai Y, Rizzuto R, Klotz KN, Leung E, Mac Lennan S, Baraldi PG, Borea PA. Gessi S, et al. Mol Pharmacol. 2005 Jun;67(6):2137-47. doi: 10.1124/mol.104.009225. Epub 2005 Mar 23. Mol Pharmacol. 2005. PMID: 15788741

Pharmacological characterization of novel adenosine ligands in recombinant and native human A2B receptors.

Varani K, Gessi S, Merighi S, Vincenzi F, Cattabriga E, Benini A, Klotz KN, Baraldi PG, Tabrizi MA, Lennan SM, Leung E, Borea PA. Varani K, et al. Biochem Pharmacol. 2005 Nov 25;70(11):1601-12. doi: 10.1016/j.bcp.2005.08.018. Epub 2005 Oct 10. Biochem Pharmacol. 2005. PMID: 16219300

Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.

Carotti A, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, Nieto R, Raviña E, Sanz F, Segarra V, Sotelo E, Stefanachi A, Vidal B. Carotti A, et al. J Med Chem. 2006 Jan 12;49(1):282-99. doi: 10.1021/jm0506221. J Med Chem. 2006. PMID: 16392813

1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.

Fernández F, Caamaño O, Isabel Nieto M, López C, García-Mera X, Stefanachi A, Nicolotti O, Isabel Loza M, Brea J, Esteve C, Segarra V, Vidal B, Carotti A. Fernández F, et al. Bioorg Med Chem. 2009 May 15;17(10):3618-29. doi: 10.1016/j.bmc.2009.03.062. Epub 2009 Apr 5. Bioorg Med Chem. 2009. PMID: 19398343

1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships.

Stefanachi A, Nicolotti O, Leonetti F, Cellamare S, Campagna F, Loza MI, Brea JM, Mazza F, Gavuzzo E, Carotti A. Stefanachi A, et al. Bioorg Med Chem. 2008 Nov 15;16(22):9780-9. doi: 10.1016/j.bmc.2008.09.067. Epub 2008 Sep 30. Bioorg Med Chem. 2008. PMID: 18938084

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