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Page 1
Structure based design of 4-(3-aminomethylphenyl)piperidinyl-1-amides: novel, potent, selective, and orally bioavailable inhibitors of betaII tryptase.
Levell J, Astles P, Eastwood P, Cairns J, Houille O, Aldous S, Merriman G, Whiteley B, Pribish J, Czekaj M, Liang G, Maignan S, Guilloteau JP, Dupuy A, Davidson J, Harrison T, Morley A, Watson S, Fenton G, McCarthy C, Romano J, Mathew R, Engers D, Gardyan M, Sides K, Kwong J, Tsay J, Rebello S, Shen L, Wang J, Luo Y, Giardino O, Lim HK, Smith K, Pauls H. Levell J, et al. Among authors: maignan s. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
Discovery of an orally efficacious inhibitor of coagulation factor Xa which incorporates a neutral P1 ligand.
Choi-Sledeski YM, Kearney R, Poli G, Pauls H, Gardner C, Gong Y, Becker M, Davis R, Spada A, Liang G, Chu V, Brown K, Collussi D, Leadley R Jr, Rebello S, Moxey P, Morgan S, Bentley R, Kasiewski C, Maignan S, Guilloteau JP, Mikol V. Choi-Sledeski YM, et al. Among authors: maignan s. J Med Chem. 2003 Feb 27;46(5):681-4. doi: 10.1021/jm020384z. J Med Chem. 2003. PMID: 12593648
Novel pyrazinone inhibitors of mast cell tryptase: synthesis and SAR evaluation.
Hopkins C, Neuenschwander K, Scotese A, Jackson S, Nieduzak T, Pauls H, Liang G, Sides K, Cramer D, Cairns J, Maignan S, Mathieu M. Hopkins C, et al. Among authors: maignan s. Bioorg Med Chem Lett. 2004 Oct 4;14(19):4819-23. doi: 10.1016/j.bmcl.2004.07.051. Bioorg Med Chem Lett. 2004. PMID: 15341931
Structure-based library design and the discovery of a potent and selective mast cell β-tryptase inhibitor as an oral therapeutic agent.
Liang G, Aldous S, Merriman G, Levell J, Pribish J, Cairns J, Chen X, Maignan S, Mathieu M, Tsay J, Sides K, Rebello S, Whitely B, Morize I, Pauls HW. Liang G, et al. Among authors: maignan s. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1049-54. doi: 10.1016/j.bmcl.2011.11.119. Epub 2011 Dec 7. Bioorg Med Chem Lett. 2012. PMID: 22192588
Design and structure-activity relationships of potent and selective inhibitors of blood coagulation factor Xa.
Ewing WR, Becker MR, Manetta VE, Davis RS, Pauls HW, Mason H, Choi-Sledeski YM, Green D, Cha D, Spada AP, Cheney DL, Mason JS, Maignan S, Guilloteau JP, Brown K, Colussi D, Bentley R, Bostwick J, Kasiewski CJ, Morgan SR, Leadley RJ, Dunwiddie CT, Perrone MH, Chu V. Ewing WR, et al. Among authors: maignan s. J Med Chem. 1999 Sep 9;42(18):3557-71. doi: 10.1021/jm990040h. J Med Chem. 1999. PMID: 10479288
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization.
Choi-Sledeski YM, McGarry DG, Green DM, Mason HJ, Becker MR, Davis RS, Ewing WR, Dankulich WP, Manetta VE, Morris RL, Spada AP, Cheney DL, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Leadley RJ, Maignan S, Guilloteau JP, Dunwiddie CT, Pauls HW. Choi-Sledeski YM, et al. Among authors: maignan s. J Med Chem. 1999 Sep 9;42(18):3572-87. doi: 10.1021/jm990041+. J Med Chem. 1999. PMID: 10479289
Design of potent IGF1-R inhibitors related to bis-azaindoles.
Nemecek C, Metz WA, Wentzler S, Ding FX, Venot C, Souaille C, Dagallier A, Maignan S, Guilloteau JP, Bernard F, Henry A, Grapinet S, Lesuisse D. Nemecek C, et al. Among authors: maignan s. Chem Biol Drug Des. 2010 Aug;76(2):100-6. doi: 10.1111/j.1747-0285.2010.00991.x. Epub 2010 Jun 9. Chem Biol Drug Des. 2010. PMID: 20545947
Discovery of the first non-ATP competitive IGF-1R kinase inhibitors: advantages in comparison with competitive inhibitors.
Lesuisse D, Mauger J, Nemecek C, Maignan S, Boiziau J, Harlow G, Hittinger A, Ruf S, Strobel H, Nair A, Ritter K, Malleron JL, Dagallier A, El-Ahmad Y, Guilloteau JP, Guizani H, Bouchard H, Venot C. Lesuisse D, et al. Among authors: maignan s. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2224-8. doi: 10.1016/j.bmcl.2011.03.003. Epub 2011 Mar 4. Bioorg Med Chem Lett. 2011. PMID: 21441024
22 results