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A carboxylic acid isostere screen of the DHODH inhibitor Brequinar.
DeRatt LG, Christine Pietsch E, Tanner A, Shaffer P, Jacoby E, Wang W, Kazmi F, Zhang X, Attar RM, Edwards JP, Kuduk SD. DeRatt LG, et al. Among authors: jacoby e. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127589. doi: 10.1016/j.bmcl.2020.127589. Epub 2020 Sep 29. Bioorg Med Chem Lett. 2020. PMID: 33007394
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Ostermann N, Ruedisser S, Ehrhardt C, Breitenstein W, Marzinzik A, Jacoby E, Vangrevelinghe E, Ottl J, Klumpp M, Hartwieg JC, Cumin F, Hassiepen U, Trappe J, Sedrani R, Geisse S, Gerhartz B, Richert P, Francotte E, Wagner T, Krömer M, Kosaka T, Webb RL, Rigel DF, Maibaum J, Baeschlin DK. Ostermann N, et al. Among authors: jacoby e. J Med Chem. 2013 Mar 28;56(6):2196-206. doi: 10.1021/jm301706j. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23360239
Structural investigation of B-Raf paradox breaker and inducer inhibitors.
Arora R, Di Michele M, Stes E, Vandermarliere E, Martens L, Gevaert K, Van Heerde E, Linders JT, Brehmer D, Jacoby E, Bonnet P. Arora R, et al. Among authors: jacoby e. J Med Chem. 2015 Feb 26;58(4):1818-31. doi: 10.1021/jm501667n. Epub 2015 Feb 10. J Med Chem. 2015. PMID: 25611072
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. Among authors: jacoby e. J Med Chem. 2013 Mar 28;56(6):2207-17. doi: 10.1021/jm3017078. Epub 2013 Mar 15. J Med Chem. 2013. PMID: 23425156
Molecular lipophilicity in protein modeling and drug design.
Efremov RG, Chugunov AO, Pyrkov TV, Priestle JP, Arseniev AS, Jacoby E. Efremov RG, et al. Among authors: jacoby e. Curr Med Chem. 2007;14(4):393-415. doi: 10.2174/092986707779941050. Curr Med Chem. 2007. PMID: 17305542 Review.
208 results