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Publikationer i urvalet

18 träffar

Bibliografisk träff 2022-07-22

High ligand efficiency quinazoline compounds as novel A2A adenosine receptor antagonists.

Bolteau R, Duroux R, Laversin A, Vreulz B, Shiriaeva A, Stauch B, Han GW, Cherezov V, Renault N, Barczyk A, Ravez S, Coevoet M, Melnyk P, Liberelle M, Yous S.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2022.114620

Bibliografisk träff 2021-10-13

Adenosine receptor antagonists: Recent advances and therapeutic perspective.

Saini A, Patel R, Gaba S, Singh G, Gupta GD, Monga V.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2021.113907

Bibliografisk träff 2021-06-09

Adenosine A2AR/A1R Antagonists Enabling Additional H3R Antagonism for the Treatment of Parkinson's Disease.

Hagenow S, Affini A, Pioli EY, Hinz S, Zhao Y, Porras G, Namasivayam V, Müller CE, Lin JS, Bezard E, Stark H.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.0c00914

Bibliografisk träff 2020-07-30

Adenosine A2A Receptor Antagonists for Cancer Immunotherapy.

Yu F, Zhu C, Xie Q, Wang Y.

J Med Chem · research support, non-u.s. gov't; review; journal article · DOI 10.1021/acs.jmedchem.0c00237

Bibliografisk träff 2019-02-18

Pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines to develop functionalized ligands to target adenosine receptors: fluorescent ligands as an example.

Federico S, Margiotta E, Paoletta S, Kachler S, Klotz KN, Jacobson KA, Pastorin G, Moro S, Spalluto G.

Medchemcomm · research-article; journal article · DOI 10.1039/c9md00014c

Bibliografisk träff 2017-12-09

Identification of novel small-molecule inhibitors of Zika virus infection.

Micewicz ED, Khachatoorian R, French SW, Ruchala P.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2017.12.019

Bibliografisk träff 2017-12-05

Antagonists of the adenosine A2A receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity.

Duroux R, Agouridas L, Renault N, El Bakali J, Furman C, Melnyk P, Yous S.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.12.007

Bibliografisk träff 2014-12-02

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

Morris LC, Nance KD, Gentry PR, Days EL, Weaver CD, Niswender CM, Thompson AD, Jones CK, Locuson CW, Morrison RD, Daniels JS, Niswender KD, Lindsley CW.

J Med Chem · research support, non-u.s. gov't; rapid-communication; journal article; research support, n.i.h., extramural · DOI 10.1021/jm501375c

Bibliografisk träff 2013-12-01

Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists.

Yang Z, Li X, Ma H, Zheng J, Zhen X, Zhang X.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2013.11.051

Bibliografisk träff 2013-11-15

Adenosine A2A receptor as a drug discovery target.

de Lera Ruiz M, Lim YH, Zheng J.

J Med Chem · review; journal article · DOI 10.1021/jm4011669

Bibliografisk träff 2013-05-30

Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.

Stössel A, Schlenk M, Hinz S, Küppers P, Heer J, Gütschow M, Müller CE.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm400336x

Bibliografisk träff 2011-06-10

Biophysical mapping of the adenosine A2A receptor.

Zhukov A, Andrews SP, Errey JC, Robertson N, Tehan B, Mason JS, Marshall FH, Weir M, Congreve M.

J Med Chem · research-article; journal article · DOI 10.1021/jm2003798

Bibliografisk träff 2011-02-24

Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones.

Harris JM, Neustadt BR, Zhang H, Lachowicz J, Cohen-Williams M, Varty G, Hao J, Stamford AW.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2011.02.045

Bibliografisk träff 2011-01-06

Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.

Sams AG, Mikkelsen GK, Larsen M, Langgård M, Howells ME, Schrøder TJ, Brennum LT, Torup L, Jørgensen EB, Bundgaard C, Kreilgård M, Bang-Andersen B.

J Med Chem · journal article · DOI 10.1021/jm1008659

Bibliografisk träff 2010-07-24

Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.

Sams AG, Mikkelsen GK, Larsen M, Torup L, Brennum LT, Schrøder TJ, Bang-Andersen B.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2010.06.138

Bibliografisk träff 2008-11-24

Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines.

Neustadt BR, Liu H, Hao J, Greenlee WJ, Stamford AW, Foster C, Arik L, Lachowicz J, Zhang H, Bertorelli R, Fredduzzi S, Varty G, Cohen-Williams M, Ng K.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2008.11.075

Bibliografisk träff 2008-01-12

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 · journal article · DOI 10.1021/jm070623o

Bibliografisk träff 2006-12-03

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 · journal article · DOI 10.1016/j.bmcl.2006.11.083

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Publikationer i urvalet

High ligand efficiency quinazoline compounds as novel A<sub>2A</sub> adenosine receptor antagonists.

Adenosine receptor antagonists: Recent advances and therapeutic perspective.

Adenosine A<sub>2A</sub>R/A<sub>1</sub>R Antagonists Enabling Additional H<sub>3</sub>R Antagonism for the Treatment of Parkinson's Disease.

Adenosine A<sub>2A</sub> Receptor Antagonists for Cancer Immunotherapy.

Pyrazolo[4,3-<i>e</i>][1,2,4]triazolo[1,5-<i>c</i>]pyrimidines to develop functionalized ligands to target adenosine receptors: fluorescent ligands as an example.

Identification of novel small-molecule inhibitors of Zika virus infection.

Antagonists of the adenosine A<sub>2A</sub> receptor based on a 2-arylbenzoxazole scaffold: Investigation of the C5- and C7-positions to enhance affinity.

Discovery of (S)-2-cyclopentyl-N-((1-isopropylpyrrolidin2-yl)-9-methyl-1-oxo-2,9-dihydro-1H-pyrrido[3,4-b]indole-4-carboxamide (VU0453379): a novel, CNS penetrant glucagon-like peptide 1 receptor (GLP-1R) positive allosteric modulator (PAM).

Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists.

Adenosine A2A receptor as a drug discovery target.

Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.

Biophysical mapping of the adenosine A2A receptor.

Potent and selective adenosine A(2A) receptor antagonists: [1,2,4]-triazolo[4,3-c]pyrimidin-3-ones.

Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.

Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.

Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines.

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

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