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Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.
Hudkins RL, Aimone LD, Bailey TR, Bendesky RJ, Dandu RR, Dunn D, Gruner JA, Josef KA, Lin YG, Lyons J, Marcy VR, Mathiasen JR, Sundar BG, Tao M, Zulli AL, Raddatz R, Bacon ER. Hudkins RL, et al. Among authors: josef ka. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5493-7. doi: 10.1016/j.bmcl.2011.06.108. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21782432
Mixed-lineage kinase 1 and mixed-lineage kinase 3 subtype-selective dihydronaphthyl[3,4-a]pyrrolo[3,4-c]carbazole-5-ones: optimization, mixed-lineage kinase 1 crystallography, and oral in vivo activity in 1-methyl-4-phenyltetrahydropyridine models.
Hudkins RL, Diebold JL, Tao M, Josef KA, Park CH, Angeles TS, Aimone LD, Husten J, Ator MA, Meyer SL, Holskin BP, Durkin JT, Fedorov AA, Fedorov EV, Almo SC, Mathiasen JR, Bozyczko-Coyne D, Saporito MS, Scott RW, Mallamo JP. Hudkins RL, et al. Among authors: josef ka. J Med Chem. 2008 Sep 25;51(18):5680-9. doi: 10.1021/jm8005838. Epub 2008 Aug 21. J Med Chem. 2008. PMID: 18714982
4,5-dihydropyridazin-3-one derivatives as histamine H₃ receptor inverse agonists.
Hudkins RL, Aimone LD, Dandu RR, Dunn D, Gruner JA, Huang Z, Josef KA, Lyons JA, Mathiasen JR, Tao M, Zulli AL, Raddatz R. Hudkins RL, et al. Among authors: josef ka. Bioorg Med Chem Lett. 2012 Jan 1;22(1):194-8. doi: 10.1016/j.bmcl.2011.11.037. Epub 2011 Nov 16. Bioorg Med Chem Lett. 2012. PMID: 22142542
Discovery of (1R,6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]-3,4-diaza-bicyclo[4.1.0]hept-4-en-2-one (R,S-4a): histamine H(3) receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity.
Hudkins RL, Josef KA, Becknell NC, Aimone LD, Lyons JA, Mathiasen JR, Gruner JA, Raddatz R. Hudkins RL, et al. Among authors: josef ka. Bioorg Med Chem Lett. 2014 Mar 1;24(5):1303-6. doi: 10.1016/j.bmcl.2014.01.061. Epub 2014 Jan 30. Bioorg Med Chem Lett. 2014. PMID: 24513042
D-amino acid containing, high-affinity inhibitors of recombinant human calpain I.
Chatterjee S, Gu ZQ, Dunn D, Tao M, Josef K, Tripathy R, Bihovsky R, Senadhi SE, O'Kane TM, McKenna BA, Mallya S, Ator MA, Bozyczko-Coyne D, Siman R, Mallamo JP. Chatterjee S, et al. J Med Chem. 1998 Jul 16;41(15):2663-6. doi: 10.1021/jm980035y. J Med Chem. 1998. PMID: 9667954 No abstract available.
15 results