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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: guilloteau jp. Bioorg Med Chem. 2005 Apr 15;13(8):2859-72. doi: 10.1016/j.bmc.2005.02.014. Bioorg Med Chem. 2005. PMID: 15781396
Optimization of the beta-aminoester class of factor Xa inhibitors. Part 2: Identification of FXV673 as a potent and selective inhibitor with excellent In vivo anticoagulant activity.
Guertin KR, Gardner CJ, Klein SI, Zulli AL, Czekaj M, Gong Y, Spada AP, Cheney DL, Maignan S, Guilloteau JP, Brown KD, Colussi DJ, Chu V, Heran CL, Morgan SR, Bentley RG, Dunwiddie CT, Leadley RJ, Pauls HW. Guertin KR, et al. Among authors: guilloteau jp. Bioorg Med Chem Lett. 2002 Jun 17;12(12):1671-4. doi: 10.1016/s0960-894x(02)00213-5. Bioorg Med Chem Lett. 2002. PMID: 12039587
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: guilloteau jp. J Med Chem. 2003 Feb 27;46(5):681-4. doi: 10.1021/jm020384z. J Med Chem. 2003. PMID: 12593648
Design, synthesis and characterization of a novel class of coumarin-based inhibitors of inducible nitric oxide synthase.
Jackson SA, Sahni S, Lee L, Luo Y, Nieduzak TR, Liang G, Chiang Y, Collar N, Fink D, He W, Laoui A, Merrill J, Boffey R, Crackett P, Rees B, Wong M, Guilloteau JP, Mathieu M, Rebello SS. Jackson SA, et al. Among authors: guilloteau jp. Bioorg Med Chem. 2005 Apr 15;13(8):2723-39. doi: 10.1016/j.bmc.2005.02.036. Bioorg Med Chem. 2005. PMID: 15781384
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: guilloteau jp. J Med Chem. 1999 Sep 9;42(18):3557-71. doi: 10.1021/jm990040h. J Med Chem. 1999. PMID: 10479288
Crystal structures of human factor Xa complexed with potent inhibitors.
Maignan S, Guilloteau JP, Pouzieux S, Choi-Sledeski YM, Becker MR, Klein SI, Ewing WR, Pauls HW, Spada AP, Mikol V. Maignan S, et al. Among authors: guilloteau jp. J Med Chem. 2000 Aug 24;43(17):3226-32. doi: 10.1021/jm000940u. J Med Chem. 2000. PMID: 10966741
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: guilloteau jp. J Med Chem. 1999 Sep 9;42(18):3572-87. doi: 10.1021/jm990041+. J Med Chem. 1999. PMID: 10479289
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: guilloteau jp. 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
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: guilloteau jp. 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
17 results