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Page 1
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 1).
Tremont SJ, Lee LF, Huang HC, Keller BT, Banerjee SC, Both SR, Carpenter AJ, Wang CC, Garland DJ, Huang W, Jones C, Koeller KJ, Kolodziej SA, Li J, Manning RE, Mahoney MW, Miller RE, Mischke DA, Rath NP, Fletcher T, Reinhard EJ, Tollefson MB, Vernier WF, Wagner GM, Rapp SR, Beaudry J, Glenn K, Regina K, Schuh JR, Smith ME, Trivedi JS, Reitz DB. Tremont SJ, et al. Among authors: tollefson mb. J Med Chem. 2005 Sep 8;48(18):5837-52. doi: 10.1021/jm040215+. J Med Chem. 2005. PMID: 16134950
Discovery of a simple picomolar inhibitor of cholesteryl ester transfer protein.
Reinhard EJ, Wang JL, Durley RC, Fobian YM, Grapperhaus ML, Hickory BS, Massa MA, Norton MB, Promo MA, Tollefson MB, Vernier WF, Connolly DT, Witherbee BJ, Melton MA, Regina KJ, Smith ME, Sikorski JA. Reinhard EJ, et al. Among authors: tollefson mb. J Med Chem. 2003 May 22;46(11):2152-68. doi: 10.1021/jm020528+. J Med Chem. 2003. PMID: 12747787
Discovery of potent, nonsystemic apical sodium-codependent bile acid transporter inhibitors (Part 2).
Huang HC, Tremont SJ, Lee LF, Keller BT, Carpenter AJ, Wang CC, Banerjee SC, Both SR, Fletcher T, Garland DJ, Huang W, Jones C, Koeller KJ, Kolodziej SA, Li J, Manning RE, Mahoney MW, Miller RE, Mischke DA, Rath NP, Reinhard EJ, Tollefson MB, Vernier WF, Wagner GM, Rapp SR, Beaudry J, Glenn K, Regina K, Schuh JR, Smith ME, Trivedi JS, Reitz DB. Huang HC, et al. Among authors: tollefson mb. J Med Chem. 2005 Sep 8;48(18):5853-68. doi: 10.1021/jm0402162. J Med Chem. 2005. PMID: 16134951
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: tollefson mb. J Med Chem. 2010 Mar 25;53(6):2656-60. doi: 10.1021/jm901781q. J Med Chem. 2010. PMID: 20196613
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: tollefson mb. 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
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: tollefson mb. 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
13 results