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Publikationer i urvalet

32 träffar

Bibliografisk träff 2023-09-14

Discovery and Characterization of Novel CNS-Penetrant GPR55 Agonists.

Hewer RC, Christie LA, Doyle KJ, Xu X, Roberts MJ, Dickson L, Cheung T, Cadwalladr DH, Pickford P, Teall M, Powell JAC, Sheardown S, Narayana L, Brice NL, Dawson LA, Carlton M, Bürli RW.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.3c00784

Bibliografisk träff 2023-07-19

A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.

Sutherland JJ, Yonchev D, Fekete A, Urban L.

Nat Commun · research support, non-u.s. gov't; research-article; journal article · DOI 10.1038/s41467-023-40064-9

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 2021-04-16

First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate.

Sun H, Monenschein H, Schiffer HH, Reichard HA, Kikuchi S, Hopkins M, Macklin TK, Hitchcock S, Adams M, Green J, Brown J, Murphy ST, Kaushal N, Collia DR, Moore S, Ray WJ, English NM, Carlton MBL, Brice NL.

J Med Chem · journal article · DOI 10.1021/acs.jmedchem.0c02081

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 2020-07-29

New drug approvals for 2019: Synthesis and clinical applications.

Yuan S, Yu B, Liu HM.

Eur J Med Chem · review; journal article · DOI 10.1016/j.ejmech.2020.112667

Bibliografisk träff 2019-02-02

Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.

Załuski M, Schabikowski J, Schlenk M, Olejarz-Maciej A, Kubas B, Karcz T, Kuder K, Latacz G, Zygmunt M, Synak D, Hinz S, Müller CE, Kieć-Kononowicz K.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2019.02.004

Bibliografisk träff 2018-11-24

Discovery of monoamine oxidase inhibitors by medicinal chemistry approaches.

Hong R, Li X.

Medchemcomm · review-article; review; journal article · DOI 10.1039/c8md00446c

Bibliografisk träff 2018-05-14

Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.

Załuski M, Stanuch K, Karcz T, Hinz S, Latacz G, Szymańska E, Schabikowski J, Doroż-Płonka A, Handzlik J, Drabczyńska A, Müller CE, Kieć-Kononowicz K.

Medchemcomm · research-article; journal article · DOI 10.1039/c8md00070k

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 2015-09-07

1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor.

Van der Walt MM, Terre'Blanche G.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2015.09.012

Bibliografisk träff 2015-02-07

Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.

Mikkelsen GK, Langgård M, Schrøder TJ, Kreilgaard M, Jørgensen EB, Brandt G, Griffon Y, Boffey R, Bang-Andersen B.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2015.01.062

Bibliografisk träff 2014-04-28

8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists.

Endo K, Deguchi K, Matsunaga H, Tomaya K, Yamada K.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2014.04.041

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 2013-09-28

Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies.

Thomas R, Lee J, Chevalier V, Sadler S, Selesniemi K, Hatfield S, Sitkovsky M, Ondrechen MJ, Jones GB.

Bioorg Med Chem · research-article; journal article · DOI 10.1016/j.bmc.2013.09.043

Bibliografisk träff 2013-09-25

1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.

Koch P, Akkari R, Brunschweiger A, Borrmann T, Schlenk M, Küppers P, Köse M, Radjainia H, Hockemeyer J, Drabczyńska A, Kieć-Kononowicz K, Müller CE.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2013.09.044

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 2013-04-02

Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.

Jörg M, Shonberg J, Mak FS, Miller ND, Yuriev E, Scammells PJ, Capuano B.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2013.03.070

Bibliografisk träff 2013-01-16

Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.

Rivara S, Piersanti G, Bartoccini F, Diamantini G, Pala D, Riccioni T, Stasi MA, Cabri W, Borsini F, Mor M, Tarzia G, Minetti P.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm301686s

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 2011-05-23

Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.

Drabczyńska A, Yuzlenko O, Köse M, Paskaleva M, Schiedel AC, Karolak-Wojciechowska J, Handzlik J, Karcz T, Kuder K, Müller CE, Kieć-Kononowicz K.

Eur J Med Chem · research support, non-u.s. gov't; validation study; journal article · DOI 10.1016/j.ejmech.2011.05.023

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 2010-10-25

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 · journal article · DOI 10.1021/jm100971t

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 2009-04-01

Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.

Gillespie RJ, Bamford SJ, Gaur S, Jordan AM, Lerpiniere J, Mansell HL, Stratton GC.

Bioorg Med Chem Lett · journal article · DOI 10.1016/j.bmcl.2009.03.142

Bibliografisk träff 2009-01-01

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 · journal article · DOI 10.1021/jm800961g

Bibliografisk träff 2008-08-05

Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues.

Pretorius J, Malan SF, Castagnoli N, Bergh JJ, Petzer JP.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2008.07.088

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 2007-08-22

Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands.

Drabczyńska A, Müller CE, Schiedel A, Schumacher B, Karolak-Wojciechowska J, Fruziński A, Zobnina W, Yuzlenko O, Kieć-Kononowicz K.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2007.07.051

Gå till forskningen.

Publikationer i urvalet

Discovery and Characterization of Novel CNS-Penetrant GPR55 Agonists.

A preclinical secondary pharmacology resource illuminates target-adverse drug reaction associations of marketed drugs.

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

Adenosine receptor antagonists: Recent advances and therapeutic perspective.

First-Time Disclosure of CVN424, a Potent and Selective GPR6 Inverse Agonist for the Treatment of Parkinson's Disease: Discovery, Pharmacological Validation, and Identification of a Clinical Candidate.

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

New drug approvals for 2019: Synthesis and clinical applications.

Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.

Discovery of monoamine oxidase inhibitors by medicinal chemistry approaches.

Tricyclic xanthine derivatives containing a basic substituent: adenosine receptor affinity and drug-related properties.

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.

1,3,7-Triethyl-substituted xanthines--possess nanomolar affinity for the adenosine A1 receptor.

Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.

8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists.

Adenosine A2A receptor as a drug discovery target.

Design and evaluation of xanthine based adenosine receptor antagonists: potential hypoxia targeted immunotherapies.

1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.

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

Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.

Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors.

Biophysical mapping of the adenosine A2A receptor.

Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.

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.

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

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

Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.

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

Dual inhibition of monoamine oxidase B and antagonism of the adenosine A(2A) receptor by (E,E)-8-(4-phenylbutadien-1-yl)caffeine analogues.

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

Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands.