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Page 1
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 1: design, synthesis and structure-activity relationship studies.
Vergne F, Bernardelli P, Lorthiois E, Pham N, Proust E, Oliveira C, Mafroud AK, Royer F, Wrigglesworth R, Schellhaas J, Barvian M, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Berna P, Soulard P. Vergne F, et al. Among authors: lorthiois e. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4607-13. doi: 10.1016/j.bmcl.2004.07.008. Bioorg Med Chem Lett. 2004. PMID: 15324874
Discovery of thiadiazoles as a novel structural class of potent and selective PDE7 inhibitors. Part 2: metabolism-directed optimization studies towards orally bioavailable derivatives.
Vergne F, Bernardelli P, Lorthiois E, Pham N, Proust E, Oliveira C, Mafroud AK, Ducrot P, Wrigglesworth R, Berlioz-Seux F, Coleon F, Chevalier E, Moreau F, Idrissi M, Tertre A, Descours A, Berna P, Li M. Vergne F, et al. Among authors: lorthiois e. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4615-21. doi: 10.1016/j.bmcl.2004.07.009. Bioorg Med Chem Lett. 2004. PMID: 15324875
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 1.
Lorthiois E, Bernardelli P, Vergne F, Oliveira C, Mafroud AK, Proust E, Heuze L, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Wrigglesworth R, Descours A, Soulard P, Berna P. Lorthiois E, et al. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4623-6. doi: 10.1016/j.bmcl.2004.07.011. Bioorg Med Chem Lett. 2004. PMID: 15324876
Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives.
Bernardelli P, Lorthiois E, Vergne F, Oliveira C, Mafroud AK, Proust E, Pham N, Ducrot P, Moreau F, Idrissi M, Tertre A, Bertin B, Coupe M, Chevalier E, Descours A, Berlioz-Seux F, Berna P, Li M. Bernardelli P, et al. Among authors: lorthiois e. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4627-31. doi: 10.1016/j.bmcl.2004.07.010. Bioorg Med Chem Lett. 2004. PMID: 15324877
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Lorthiois E, Breitenstein W, Cumin F, Ehrhardt C, Francotte E, Jacoby E, Ostermann N, Sellner H, Kosaka T, Webb RL, Rigel DF, Hassiepen U, Richert P, Wagner T, Maibaum J. Lorthiois E, et al. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
Design, Synthesis, and Preclinical Characterization of Selective Factor D Inhibitors Targeting the Alternative Complement Pathway.
Karki RG, Powers J, Mainolfi N, Anderson K, Belanger DB, Liu D, Ji N, Jendza K, Gelin CF, Mac Sweeney A, Solovay C, Delgado O, Crowley M, Liao SM, Argikar UA, Flohr S, La Bonte LR, Lorthiois EL, Vulpetti A, Brown A, Long D, Prentiss M, Gradoux N, de Erkenez A, Cumin F, Adams C, Jaffee B, Mogi M. Karki RG, et al. Among authors: lorthiois el. J Med Chem. 2019 May 9;62(9):4656-4668. doi: 10.1021/acs.jmedchem.9b00271. Epub 2019 Apr 30. J Med Chem. 2019. PMID: 30995036
Structure-Based Design and Preclinical Characterization of Selective and Orally Bioavailable Factor XIa Inhibitors: Demonstrating the Power of an Integrated S1 Protease Family Approach.
Lorthiois E, Roache J, Barnes-Seeman D, Altmann E, Hassiepen U, Turner G, Duvadie R, Hornak V, Karki RG, Schiering N, Weihofen WA, Perruccio F, Calhoun A, Fazal T, Dedic D, Durand C, Dussauge S, Fettis K, Tritsch F, Dentel C, Druet A, Liu D, Kirman L, Lachal J, Namoto K, Bevan D, Mo R, Monnet G, Muller L, Zessis R, Huang X, Lindsley L, Currie T, Chiu YH, Fridrich C, Delgado P, Wang S, Hollis-Symynkywicz M, Berghausen J, Williams E, Liu H, Liang G, Kim H, Hoffmann P, Hein A, Ramage P, D'Arcy A, Harlfinger S, Renatus M, Ruedisser S, Feldman D, Elliott J, Sedrani R, Maibaum J, Adams CM. Lorthiois E, et al. J Med Chem. 2020 Aug 13;63(15):8088-8113. doi: 10.1021/acs.jmedchem.0c00279. Epub 2020 Jul 21. J Med Chem. 2020. PMID: 32551603
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J. Lorthiois E, et al. J Med Chem. 2017 Jul 13;60(13):5717-5735. doi: 10.1021/acs.jmedchem.7b00425. Epub 2017 Jun 30. J Med Chem. 2017. PMID: 28621538
19 results