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Page 1
Optimization of LpxC Inhibitors for Antibacterial Activity and Cardiovascular Safety.
Cohen F, Aggen JB, Andrews LD, Assar Z, Boggs J, Choi T, Dozzo P, Easterday AN, Haglund CM, Hildebrandt DJ, Holt MC, Joly K, Jubb A, Kamal Z, Kane TR, Konradi AW, Krause KM, Linsell MS, Machajewski TD, Miroshnikova O, Moser HE, Nieto V, Phan T, Plato C, Serio AW, Seroogy J, Shakhmin A, Stein AJ, Sun AD, Sviridov S, Wang Z, Wlasichuk K, Yang W, Zhou X, Zhu H, Cirz RT. Cohen F, et al. Among authors: konradi aw. ChemMedChem. 2019 Aug 20;14(16):1560-1572. doi: 10.1002/cmdc.201900287. Epub 2019 Aug 5. ChemMedChem. 2019. PMID: 31283109
Selective and brain-permeable polo-like kinase-2 (Plk-2) inhibitors that reduce α-synuclein phosphorylation in rat brain.
Aubele DL, Hom RK, Adler M, Galemmo RA Jr, Bowers S, Truong AP, Pan H, Beroza P, Neitz RJ, Yao N, Lin M, Tonn G, Zhang H, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Diep L, Fitzgerald K, Hoffman J, Motter R, Fauss D, Tanaka P, Dappen M, Jagodzinski J, Chan W, Konradi AW, Latimer L, Zhu YL, Sham HL, Anderson JP, Bergeron M, Artis DR. Aubele DL, et al. Among authors: konradi aw. ChemMedChem. 2013 Aug;8(8):1295-313. doi: 10.1002/cmdc.201300166. Epub 2013 Jun 21. ChemMedChem. 2013. PMID: 23794260
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
Design, synthesis, and structure-activity relationship of novel orally efficacious pyrazole/sulfonamide based dihydroquinoline gamma-secretase inhibitors.
Truong AP, Aubele DL, Probst GD, Neitzel ML, Semko CM, Bowers S, Dressen D, Hom RK, Konradi AW, Sham HL, Garofalo AW, Keim PS, Wu J, Dappen MS, Wong K, Goldbach E, Quinn KP, Sauer JM, Brigham EF, Wallace W, Nguyen L, Hemphill SS, Bova MP, Bard F, Yednock TA, Basi G. Truong AP, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2009 Sep 1;19(17):4920-3. doi: 10.1016/j.bmcl.2009.07.092. Epub 2009 Jul 23. Bioorg Med Chem Lett. 2009. PMID: 19660943
Design and synthesis of disubstituted thiophene and thiazole based inhibitors of JNK.
Hom RK, Bowers S, Sealy JM, Truong AP, Probst GD, Neitzel ML, Neitz RJ, Fang L, Brogley L, Wu J, Konradi AW, Sham HL, Tóth G, Pan H, Yao N, Artis DR, Quinn K, Sauer JM, Powell K, Ren Z, Bard F, Yednock TA, Griswold-Prenner I. Hom RK, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7303-7. doi: 10.1016/j.bmcl.2010.10.066. Epub 2010 Oct 21. Bioorg Med Chem Lett. 2010. PMID: 21071223
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.
Sealy JM, Truong AP, Tso L, Probst GD, Aquino J, Hom RK, Jagodzinska BM, Dressen D, Wone DW, Brogley L, John V, Tung JS, Pleiss MA, Tucker JA, Konradi AW, Dappen MS, Toth G, Pan H, Ruslim L, Miller J, Bova MP, Sinha S, Quinn KP, Sauer JM. Sealy JM, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6386-91. doi: 10.1016/j.bmcl.2009.09.061. Epub 2009 Sep 19. Bioorg Med Chem Lett. 2009. PMID: 19811916
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
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
N-Bridged bicyclic sulfonamides as inhibitors of gamma-secretase.
Bowers S, Probst GD, Truong AP, Hom RK, Konradi AW, Sham HL, Garofalo AW, Wong K, Goldbach E, Quinn KP, Sauer JM, Wallace W, Nguyen L, Hemphill SS, Bova MP, Basi GS. Bowers S, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2009 Dec 15;19(24):6952-6. doi: 10.1016/j.bmcl.2009.10.060. Epub 2009 Oct 30. Bioorg Med Chem Lett. 2009. PMID: 19879755
Design and synthesis of highly selective, orally active Polo-like kinase-2 (Plk-2) inhibitors.
Bowers S, Truong AP, Ye M, Aubele DL, Sealy JM, Neitz RJ, Hom RK, Chan W, Dappen MS, Galemmo RA Jr, Konradi AW, Sham HL, Zhu YL, Beroza P, Tonn G, Zhang H, Hoffman J, Motter R, Fauss D, Tanaka P, Bova MP, Ren Z, Tam D, Ruslim L, Baker J, Pandya D, Diep L, Fitzgerald K, Artis DR, Anderson JP, Bergeron M. Bowers S, et al. Among authors: konradi aw. Bioorg Med Chem Lett. 2013 May 1;23(9):2743-9. doi: 10.1016/j.bmcl.2013.02.065. Epub 2013 Feb 24. Bioorg Med Chem Lett. 2013. PMID: 23522834
37 results