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Page 1
Design, synthesis, and biological evaluation of 3-[4-(2-hydroxyethyl)piperazin-1-yl]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one, a potent, orally active, brain penetrant inhibitor of phosphodiesterase 5 (PDE5).
Hughes RO, Rogier DJ, Jacobsen EJ, Walker JK, Macinnes A, Bond BR, Zhang LL, Yu Y, Zheng Y, Rumsey JM, Walgren JL, Curtiss SW, Fobian YM, Heasley SE, Cubbage JW, Moon JB, Brown DL, Acker BA, Maddux TM, Tollefson MB, Mischke BV, Owen DR, Freskos JN, Molyneaux JM, Benson AG, Blevis-Bal RM. Hughes RO, et al. Among authors: moon jb. J Med Chem. 2010 Mar 25;53(6):2656-60. doi: 10.1021/jm901781q. J Med Chem. 2010. PMID: 20196613
Design of potent inhibitors of human beta-secretase. Part 1.
Freskos JN, Fobian YM, Benson TE, Bienkowski MJ, Brown DL, Emmons TL, Heintz R, Laborde A, McDonald JJ, Mischke BV, Molyneaux JM, Moon JB, Mullins PB, Bryan Prince D, Paddock DJ, Tomasselli AG, Winterrowd G. Freskos JN, et al. Among authors: moon jb. Bioorg Med Chem Lett. 2007 Jan 1;17(1):73-7. doi: 10.1016/j.bmcl.2006.09.092. Epub 2006 Oct 4. Bioorg Med Chem Lett. 2007. PMID: 17046251
Design of potent inhibitors of human beta-secretase. Part 2.
Freskos JN, Fobian YM, Benson TE, Moon JB, Bienkowski MJ, Brown DL, Emmons TL, Heintz R, Laborde A, McDonald JJ, Mischke BV, Molyneaux JM, Mullins PB, Bryan Prince D, Paddock DJ, Tomasselli AG, Winterrowd G. Freskos JN, et al. Among authors: moon jb. Bioorg Med Chem Lett. 2007 Jan 1;17(1):78-81. doi: 10.1016/j.bmcl.2006.09.091. Epub 2006 Oct 4. Bioorg Med Chem Lett. 2007. PMID: 17049233
Investigation of aminopyridiopyrazinones as PDE5 inhibitors: Evaluation of modifications to the central ring system.
Hughes RO, Walker JK, Cubbage JW, Fobian YM, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Owen DR, Jacobsen EJ, Freskos JN, Molyneaux JM, Brown DL, Stallings WC, Acker BA, Maddux TM, Tollefson MB, Williams JM, Moon JB, Mischke BV, Rumsey JM, Zheng Y, Macinnes A, Bond BR, Yu Y. Hughes RO, et al. Among authors: moon jb. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4092-6. doi: 10.1016/j.bmcl.2009.06.004. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19539468
Identification, synthesis and SAR of amino substituted pyrido[3,2b]pyrazinones as potent and selective PDE5 inhibitors.
Owen DR, Walker JK, Jon Jacobsen E, Freskos JN, Hughes RO, Brown DL, Bell AS, Brown DG, Phillips C, Mischke BV, Molyneaux JM, Fobian YM, Heasley SE, Moon JB, Stallings WC, Joseph Rogier D, Fox DN, Palmer MJ, Ringer T, Rodriquez-Lens M, Cubbage JW, Blevis-Bal RM, Benson AG, Acker BA, Maddux TM, Tollefson MB, Bond BR, Macinnes A, Yu Y. Owen DR, et al. Among authors: moon jb. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4088-91. doi: 10.1016/j.bmcl.2009.06.012. Epub 2009 Jun 6. Bioorg Med Chem Lett. 2009. PMID: 19540112 Free article.
Optimization of the aminopyridopyrazinones class of PDE5 inhibitors: discovery of 3-[(trans-4-hydroxycyclohexyl)amino]-7-(6-methoxypyridin-3-yl)-1-(2-propoxyethyl)pyrido[3,4-b]pyrazin-2(1H)-one.
Hughes RO, Walker JK, Rogier DJ, Heasley SE, Blevis-Bal RM, Benson AG, Jacobsen EJ, Cubbage JW, Fobian YM, Owen DR, Freskos JN, Molyneaux JM, Brown DL, Acker BA, Maddux TM, Tollefson MB, Moon JB, Mischke BV, Rumsey JM, Zheng Y, MacInnes A, Bond BR, Yu Y. Hughes RO, et al. Among authors: moon jb. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5209-13. doi: 10.1016/j.bmcl.2009.07.019. Epub 2009 Jul 10. Bioorg Med Chem Lett. 2009. PMID: 19631533
Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.
Kortum SW, Benson TE, Bienkowski MJ, Emmons TL, Prince DB, Paddock DJ, Tomasselli AG, Moon JB, LaBorde A, TenBrink RE. Kortum SW, et al. Among authors: moon jb. Bioorg Med Chem Lett. 2007 Jun 15;17(12):3378-83. doi: 10.1016/j.bmcl.2007.03.096. Epub 2007 Apr 3. Bioorg Med Chem Lett. 2007. PMID: 17434734
Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS).
Carron CP, Trujillo JI, Olson KL, Huang W, Hamper BC, Dice T, Neal BE, Pelc MJ, Day JE, Rohrer DC, Kiefer JR, Moon JB, Schweitzer BA, Blake TD, Turner SR, Woerndle R, Case BL, Bono CP, Dilworth VM, Funckes-Shippy CL, Hood BL, Jerome GM, Kornmeier CM, Radabaugh MR, Williams ML, Davies MS, Wegner CD, Welsch DJ, Abraham WM, Warren CJ, Dowty ME, Hua F, Zutshi A, Yang JZ, Thorarensen A. Carron CP, et al. Among authors: moon jb. ACS Med Chem Lett. 2010 Feb 2;1(2):59-63. doi: 10.1021/ml900025z. eCollection 2010 May 13. ACS Med Chem Lett. 2010. PMID: 24900177 Free PMC article.
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.
Maillard MC, Hom RK, Benson TE, Moon JB, Mamo S, Bienkowski M, Tomasselli AG, Woods DD, Prince DB, Paddock DJ, Emmons TL, Tucker JA, Dappen MS, Brogley L, Thorsett ED, Jewett N, Sinha S, John V. Maillard MC, et al. Among authors: moon jb. J Med Chem. 2007 Feb 22;50(4):776-81. doi: 10.1021/jm061242y. J Med Chem. 2007. PMID: 17300163
117 results