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Items: 1 to 20 of 222

1.

Lead optimization of 4-acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A adenosine receptor antagonists for the treatment of Parkinson's disease.

Zhang X, Tellew JE, Luo Z, Moorjani M, Lin E, Lanier MC, Chen Y, Williams JP, Saunders J, Lechner SM, Markison S, Joswig T, Petroski R, Piercey J, Kargo W, Malany S, Santos M, Gross RS, Wen J, Jalali K, O'Brien Z, Stotz CE, Crespo MI, Díaz JL, Slee DH.

J Med Chem. 2008 Nov 27;51(22):7099-110. doi: 10.1021/jm800851u.

PMID:
18947224
2.
3.

Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.

Neustadt BR, Hao J, Lindo N, Greenlee WJ, Stamford AW, Tulshian D, Ongini E, Hunter J, Monopoli A, Bertorelli R, Foster C, Arik L, Lachowicz J, Ng K, Feng KI.

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1376-80. Epub 2006 Dec 3.

PMID:
17236762
4.

Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.

Slee DH, Zhang X, Moorjani M, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Wen J, O'Brien Z, Saunders J.

J Med Chem. 2008 Feb 14;51(3):400-6. doi: 10.1021/jm070623o. Epub 2008 Jan 12.

PMID:
18189346
5.

Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.

Baraldi PG, Cacciari B, Spalluto G, Bergonzoni M, Dionisotti S, Ongini E, Varani K, Borea PA.

J Med Chem. 1998 Jun 4;41(12):2126-33.

PMID:
9622554
6.

Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.

Peng H, Kumaravel G, Yao G, Sha L, Wang J, Van Vlijmen H, Bohnert T, Huang C, Vu CB, Ensinger CL, Chang H, Engber TM, Whalley ET, Petter RC.

J Med Chem. 2004 Dec 2;47(25):6218-29.

PMID:
15566292
7.

Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.

Baraldi PG, Fruttarolo F, Tabrizi MA, Preti D, Romagnoli R, El-Kashef H, Moorman A, Varani K, Gessi S, Merighi S, Borea PA.

J Med Chem. 2003 Mar 27;46(7):1229-41.

PMID:
12646033
8.

Design, synthesis, and evaluation of fused heterocyclic analogs of SCH 58261 as adenosine A2A receptor antagonists.

Shah U, Lankin CM, Boyle CD, Chackalamannil S, Greenlee WJ, Neustadt BR, Cohen-Williams ME, Higgins GA, Ng K, Varty GB, Zhang H, Lachowicz JE.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4204-9. doi: 10.1016/j.bmcl.2008.05.069. Epub 2008 May 22.

PMID:
18558486
10.

N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.

Lanier MC, Moorjani M, Luo Z, Chen Y, Lin E, Tellew JE, Zhang X, Williams JP, Gross RS, Lechner SM, Markison S, Joswig T, Kargo W, Piercey J, Santos M, Malany S, Zhao M, Petroski R, Crespo MI, Díaz JL, Saunders J, Wen J, O'Brien Z, Jalali K, Madan A, Slee DH.

J Med Chem. 2009 Feb 12;52(3):709-17. doi: 10.1021/jm800908d.

PMID:
19140664
11.

2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1.

Matasi JJ, Caldwell JP, Zhang H, Fawzi A, Cohen-Williams ME, Varty GB, Tulshian DB.

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3670-4.

PMID:
15978806
12.

Discovery of nonxanthine adenosine A2A receptor antagonists for the treatment of Parkinson's disease.

Weiss SM, Benwell K, Cliffe IA, Gillespie RJ, Knight AR, Lerpiniere J, Misra A, Pratt RM, Revell D, Upton R, Dourish CT.

Neurology. 2003 Dec 9;61(11 Suppl 6):S101-6.

PMID:
14663021
13.

Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.

Gillespie RJ, Bamford SJ, Botting R, Comer M, Denny S, Gaur S, Griffin M, Jordan AM, Knight AR, Lerpiniere J, Leonardi S, Lightowler S, McAteer S, Merrett A, Misra A, Padfield A, Reece M, Saadi M, Selwood DL, Stratton GC, Surry D, Todd R, Tong X, Ruston V, Upton R, Weiss SM.

J Med Chem. 2009 Jan 8;52(1):33-47. doi: 10.1021/jm800961g.

PMID:
19072055
14.

Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.

Shah U, Boyle CD, Chackalamannil S, Neustadt BR, Lindo N, Greenlee WJ, Foster C, Arik L, Zhai Y, Ng K, Wang S, Monopoli A, Lachowicz JE.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4199-203. doi: 10.1016/j.bmcl.2008.05.074. Epub 2008 May 22.

PMID:
18562199
15.

2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.

Moorjani M, Luo Z, Lin E, Vong BG, Chen Y, Zhang X, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Crespo MI, Díaz JL, Saunders J, Slee DH.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5402-5. doi: 10.1016/j.bmcl.2008.09.048. Epub 2008 Sep 14.

PMID:
18835161
16.

Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines.

Gillespie RJ, Cliffe IA, Dawson CE, Dourish CT, Gaur S, Jordan AM, Knight AR, Lerpiniere J, Misra A, Pratt RM, Roffey J, Stratton GC, Upton R, Weiss SM, Williamson DS.

Bioorg Med Chem Lett. 2008 May 1;18(9):2924-9. doi: 10.1016/j.bmcl.2008.03.072. Epub 2008 Mar 30.

PMID:
18411049
17.

New adenosine A2A receptor antagonists: actions on Parkinson's disease models.

Pinna A, Volpini R, Cristalli G, Morelli M.

Eur J Pharmacol. 2005 Apr 11;512(2-3):157-64.

PMID:
15840400
18.

2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs as adenosine A2A antagonists: the successful reduction of hERG activity. Part 2.

Matasi JJ, Caldwell JP, Zhang H, Fawzi A, Higgins GA, Cohen-Williams ME, Varty GB, Tulshian DB.

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3675-8.

PMID:
15982882
19.

In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.

Shook BC, Rassnick S, Osborne MC, Davis S, Westover L, Boulet J, Hall D, Rupert KC, Heintzelman GR, Hansen K, Chakravarty D, Bullington JL, Russell R, Branum S, Wells KM, Damon S, Youells S, Li X, Beauchamp DA, Palmer D, Reyes M, Demarest K, Tang Y, Rhodes K, Jackson PF.

J Med Chem. 2010 Nov 25;53(22):8104-15. doi: 10.1021/jm100971t. Epub 2010 Oct 25.

PMID:
20973483
20.

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 2. Reduction of hERG activity, observed species selectivity, and structure-activity relationships.

Slee DH, Moorjani M, Zhang X, Lin E, Lanier MC, Chen Y, Rueter JK, Lechner SM, Markison S, Malany S, Joswig T, Santos M, Gross RS, Williams JP, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Jalali K, Sai Y, Zuo Z, Yang C, Wen J, O'Brien Z, Petroski R, Saunders J.

J Med Chem. 2008 Mar 27;51(6):1730-9. doi: 10.1021/jm701187w. Epub 2008 Feb 29.

PMID:
18307293
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