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8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors.
Brunschweiger A, Koch P, Schlenk M, Rafehi M, Radjainia H, Küppers P, Hinz S, Pineda F, Wiese M, Hockemeyer J, Heer J, Denonne F, Müller CE. Brunschweiger A, et al. Among authors: heer j. Bioorg Med Chem. 2016 Nov 1;24(21):5462-5480. doi: 10.1016/j.bmc.2016.09.003. Epub 2016 Sep 3. Bioorg Med Chem. 2016. PMID: 27658798
Probing Substituents in the 1- and 3-Position: Tetrahydropyrazino-Annelated Water-Soluble Xanthine Derivatives as Multi-Target Drugs With Potent Adenosine Receptor Antagonistic Activity.
Koch P, Brunschweiger A, Namasivayam V, Ullrich S, Maruca A, Lazzaretto B, Küppers P, Hinz S, Hockemeyer J, Wiese M, Heer J, Alcaro S, Kiec-Kononowicz K, Müller CE. Koch P, et al. Among authors: heer j. Front Chem. 2018 Jun 26;6:206. doi: 10.3389/fchem.2018.00206. eCollection 2018. Front Chem. 2018. PMID: 29998095 Free PMC article.
Discovery of a novel allosteric inhibitor scaffold for polyadenosine-diphosphate-ribose polymerase 14 (PARP14) macrodomain 2.
Moustakim M, Riedel K, Schuller M, Gehring AP, Monteiro OP, Martin SP, Fedorov O, Heer J, Dixon DJ, Elkins JM, Knapp S, Bracher F, Brennan PE. Moustakim M, et al. Among authors: heer j. Bioorg Med Chem. 2018 Jul 15;26(11):2965-2972. doi: 10.1016/j.bmc.2018.03.020. Epub 2018 Mar 12. Bioorg Med Chem. 2018. PMID: 29567296 Free PMC article.
Optimization of sphingosine-1-phosphate-1 receptor agonists: effects of acidic, basic, and zwitterionic chemotypes on pharmacokinetic and pharmacodynamic profiles.
Skidmore J, Heer J, Johnson CN, Norton D, Redshaw S, Sweeting J, Hurst D, Cridland A, Vesey D, Wall I, Ahmed M, Rivers D, Myatt J, Giblin G, Philpott K, Kumar U, Stevens A, Bit RA, Haynes A, Taylor S, Watson R, Witherington J, Demont E, Heightman TD. Skidmore J, et al. Among authors: heer j. J Med Chem. 2014 Dec 26;57(24):10424-42. doi: 10.1021/jm5010336. Epub 2014 Dec 15. J Med Chem. 2014. PMID: 25431977
127 results