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Items: 1 to 20 of 41

1.

Toxicological evaluation of a novel umami flavour compound: 2-(((3-(2,3-Dimethoxyphenyl)-1H-1,2,4-triazol-5-yl)thio)methyl)pyridine.

Karanewsky DS, Arthur AJ, Liu H, Chi B, Ida L, Markison S.

Toxicol Rep. 2016 May 18;3:501-512. doi: 10.1016/j.toxrep.2016.05.002. eCollection 2016.

3.

Toxicological evaluation of a novel cooling compound: 2-(4-methylphenoxy)-N-(1H-pyrazol-3-yl)-N-(2-thienylmethyl)acetamide.

Karanewsky DS, Arthur AJ, Liu H, Chi B, Markison S.

Toxicol Rep. 2015 Sep 11;2:1291-1309. doi: 10.1016/j.toxrep.2015.09.001. eCollection 2015.

4.

Toxicological evaluation of the flavour ingredient 4-amino-5-(3-(isopropylamino)-2,2-dimethyl-3-oxopropoxy)-2-methylquinoline-3-carboxylic acid.

Arthur AJ, Karanewsky DS, Liu H, Chi B, Markison S.

Toxicol Rep. 2015 Sep 3;2:1255-1264. doi: 10.1016/j.toxrep.2015.08.012. eCollection 2015.

5.

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
6.

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
7.

Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.

Chen C, Tucci FC, Jiang W, Tran JA, Fleck BA, Hoare SR, Wen J, Chen T, Johns M, Markison S, Foster AC, Marinkovic D, Chen CW, Arellano M, Harman J, Saunders J, Bozigian H, Marks D.

Bioorg Med Chem. 2008 May 15;16(10):5606-18. doi: 10.1016/j.bmc.2008.03.072. Epub 2008 Apr 1.

PMID:
18417348
8.

Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.

Zhang X, Rueter JK, Chen Y, Moorjani M, Lanier MC, Lin E, Gross RS, Tellew JE, Williams JP, Lechner SM, Markison S, Joswig T, Malany S, Santos M, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J, Slee DH.

Bioorg Med Chem Lett. 2008 Mar 15;18(6):1778-83. doi: 10.1016/j.bmcl.2008.02.032. Epub 2008 Feb 16.

PMID:
18329269
9.

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
10.

2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents.

Slee DH, Chen Y, Zhang X, Moorjani M, Lanier MC, Lin E, Rueter JK, Williams JP, Lechner SM, Markison S, Malany S, Santos M, Gross RS, Jalali K, Sai Y, Zuo Z, Yang C, Castro-Palomino JC, Crespo MI, Prat M, Gual S, Díaz JL, Saunders J.

J Med Chem. 2008 Mar 27;51(6):1719-29. doi: 10.1021/jm701185v. Epub 2008 Feb 29.

PMID:
18307292
11.

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
12.

Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.

Chen C, Jiang W, Tran JA, Tucci FC, Fleck BA, Markison S, Wen J, Madan A, Hoare SR, Foster AC, Marinkovic D, Chen CW, Arellano M, Saunders J.

Bioorg Med Chem Lett. 2008 Jan 1;18(1):129-36. Epub 2007 Nov 4.

PMID:
18032040
13.

Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.

Tran JA, Jiang W, Tucci FC, Fleck BA, Wen J, Sai Y, Madan A, Chen TK, Markison S, Foster AC, Hoare SR, Marks D, Harman J, Chen CW, Arellano M, Marinkovic D, Bozigian H, Saunders J, Chen C.

J Med Chem. 2007 Dec 13;50(25):6356-66. Epub 2007 Nov 10.

PMID:
17994683
14.

Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.

Jiang W, Tran JA, Tucci FC, Fleck BA, Hoare SR, Markison S, Wen J, Chen CW, Marinkovic D, Arellano M, Foster AC, Chen C.

Bioorg Med Chem Lett. 2007 Dec 1;17(23):6546-52. Epub 2007 Oct 22.

PMID:
17933528
15.

Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.

Chen C, Jiang W, Tucci F, Tran JA, Fleck BA, Hoare SR, Joppa M, Markison S, Wen J, Sai Y, Johns M, Madan A, Chen T, Chen CW, Marinkovic D, Arellano M, Saunders J, Foster AC.

J Med Chem. 2007 Nov 1;50(22):5249-52. Epub 2007 Oct 5.

PMID:
17918824
16.

Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.

Jiang W, Tucci FC, Tran JA, Fleck BA, Wen J, Markison S, Marinkovic D, Chen CW, Arellano M, Hoare SR, Johns M, Foster AC, Saunders J, Chen C.

Bioorg Med Chem Lett. 2007 Oct 15;17(20):5610-3. Epub 2007 Aug 23.

PMID:
17822895
17.

Peripheral administration of the melanocortin-4 receptor antagonist NBI-12i ameliorates uremia-associated cachexia in mice.

Cheung WW, Kuo HJ, Markison S, Chen C, Foster AC, Marks DL, Mak RH.

J Am Soc Nephrol. 2007 Sep;18(9):2517-24. Epub 2007 Aug 8.

18.

Pyrrolidinones as orally bioavailable antagonists of the human melanocortin-4 receptor with anti-cachectic activity.

Tran JA, Tucci FC, Jiang W, Marinkovic D, Chen CW, Arellano M, Markison S, Fleck BA, Wen J, White NS, Pontillo J, Saunders J, Marks D, Hoare SR, Madan A, Foster AC, Chen C.

Bioorg Med Chem. 2007 Aug 1;15(15):5166-76. Epub 2007 May 17.

PMID:
17544282
19.
20.

A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties.

Dyck B, Markison S, Zhao L, Tamiya J, Grey J, Rowbottom MW, Zhang M, Vickers T, Sorensen K, Norton C, Wen J, Heise CE, Saunders J, Conlon P, Madan A, Schwarz D, Goodfellow VS.

J Med Chem. 2006 Jun 29;49(13):3753-6.

PMID:
16789729

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