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Page 1
Discovery of a potent, orally bioavailable pyrimidine VLA-4 antagonist effective in a sheep asthma model.
Semko CM, Chen L, Dressen DB, Dreyer ML, Dunn W, Farouz FS, Freedman SB, Holsztynska EJ, Jefferies M, Konradi AW, Liao A, Lugar J, Mutter L, Pleiss MA, Quinn KP, Thompson T, Thorsett ED, Vandevert C, Xu YZ, Yednock TA. Semko CM, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1741-3. doi: 10.1016/j.bmcl.2011.01.075. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316228
Synthesis, characterization and evaluation of pro-drugs of VLA-4 antagonists.
Huryn DM, Ashwell S, Baudy R, Dressen DB, Gallaway W, Grant FS, Konradi A, Ley RW, Petusky S, Pleiss MA, Sarantakis D, Semko CM, Sherman MM, Tio C, Zhang L. Huryn DM, et al. Bioorg Med Chem Lett. 2004 Apr 5;14(7):1651-4. doi: 10.1016/j.bmcl.2004.01.062. Bioorg Med Chem Lett. 2004. PMID: 15026043
Arylsulfonamide pyrimidines as VLA-4 antagonists.
Xu YZ, Konradi AW, Bard F, Dappen M, Dofiles L, Dreyer M, Gallager I, Garrido C, Krimm M, Liao Z, Messersmith E, Mutter L, Pleiss MA, Samant B, Semko CM, Smith J, Stappenbeck F, Stupi B, Vandervert C, Welch B, Wipke B, Yednock T. Xu YZ, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2013 May 15;23(10):3070-4. doi: 10.1016/j.bmcl.2013.03.010. Epub 2013 Mar 15. Bioorg Med Chem Lett. 2013. PMID: 23562062
Orally available and efficacious α4β1/α4β7 integrin inhibitors.
Xu YZ, Smith JL, Semko CM, Rossiter KI, Fukuda JY, Dappen MS, Quincy DA, Konradi AW, Mao W, Welch B, Dreyer ML, Samant B, Zhang H, Lugar J, Liao Z, Henschel C, Petersen E, Vandevert C, Shoemaker M, Wehner N, Mutter L, Shopp G, Krimm M, Chen L, Wipke B, Dofiles L, Gallager I, Sauer JM, Messersmith EK, Pleiss MA, Bard F, Yednock TA. Xu YZ, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2013 Aug 1;23(15):4370-3. doi: 10.1016/j.bmcl.2013.05.076. Epub 2013 May 31. Bioorg Med Chem Lett. 2013. PMID: 23777782
Discovery of sulfonamide-pyrazole gamma-secretase inhibitors.
Mattson MN, Neitzel ML, Quincy DA, Semko CM, Garofalo AW, Keim PS, Konradi AW, Pleiss MA, Sham HL, Brigham EF, Goldbach EG, Zhang H, Sauer JM, Basi GS. Mattson MN, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2148-50. doi: 10.1016/j.bmcl.2010.02.050. Epub 2010 Feb 14. Bioorg Med Chem Lett. 2010. PMID: 20206516
Discovery of a novel sulfonamide-pyrazolopiperidine series as potent and efficacious gamma-secretase inhibitors.
Ye XM, Konradi AW, Smith J, Xu YZ, Dressen D, Garofalo AW, Marugg J, Sham HL, Truong AP, Jagodzinski J, Pleiss M, Zhang H, Goldbach E, Sauer JM, Brigham E, Bova M, Basi GS. Ye XM, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2195-9. doi: 10.1016/j.bmcl.2010.02.039. Epub 2010 Feb 13. Bioorg Med Chem Lett. 2010. PMID: 20207136
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
Truong AP, Probst GD, Aquino J, Fang L, Brogley L, Sealy JM, Hom RK, Tucker JA, John V, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Tóth G, Yao N, Brecht E, Pan H, Artis DR, Ruslim L, Bova MP, Sinha S, Yednock TA, Zmolek W, Quinn KP, Sauer JM. Truong AP, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4789-94. doi: 10.1016/j.bmcl.2010.06.112. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20634069
Design and synthesis of a novel, orally active, brain penetrant, tri-substituted thiophene based JNK inhibitor.
Bowers S, Truong AP, Neitz RJ, Neitzel M, Probst GD, Hom RK, Peterson B, Galemmo RA Jr, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Brigham EF, Quinn KP, Sauer JM, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Bowers S, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1838-43. doi: 10.1016/j.bmcl.2011.01.046. Epub 2011 Jan 20. Bioorg Med Chem Lett. 2011. PMID: 21316234
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: prime side chromane-containing inhibitors.
Ng RA, Sun M, Bowers S, Hom RK, Probst GD, John V, Fang LY, Maillard M, Gailunas A, Brogley L, Neitz RJ, Tung JS, Pleiss MA, Konradi AW, Sham HL, Dappen MS, Adler M, Yao N, Zmolek W, Nakamura D, Quinn KP, Sauer JM, Bova MP, Ruslim L, Artis DR, Yednock TA. Ng RA, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2013 Aug 15;23(16):4674-9. doi: 10.1016/j.bmcl.2013.06.006. Epub 2013 Jun 11. Bioorg Med Chem Lett. 2013. PMID: 23856050
37 results