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Aryl 1,4-diazepane compounds as potent and selective CB2 agonists: optimization of drug-like properties and target independent parameters.
Zindell R, Walker ER, Scott J, Amouzegh P, Wu L, Ermann M, Thomson D, Fisher MB, Fullenwider CL, Grbic H, Kaplita P, Linehan B, Patel M, Patel M, Löbbe S, Block S, Albrecht C, Gemkow MJ, Shih DT, Riether D. Zindell R, et al. Among authors: ermann m. Bioorg Med Chem Lett. 2011 Jul 15;21(14):4276-80. doi: 10.1016/j.bmcl.2011.05.068. Epub 2011 May 27. Bioorg Med Chem Lett. 2011. PMID: 21689933
Arylsulfonamide CB2 receptor agonists: SAR and optimization of CB2 selectivity.
Ermann M, Riether D, Walker ER, Mushi IF, Jenkins JE, Noya-Marino B, Brewer ML, Taylor MG, Amouzegh P, East SP, Dymock BW, Gemkow MJ, Kahrs AF, Ebneth A, Löbbe S, O'Shea K, Shih DT, Thomson D. Ermann M, et al. Bioorg Med Chem Lett. 2008 Mar 1;18(5):1725-9. doi: 10.1016/j.bmcl.2008.01.042. Epub 2008 Jan 18. Bioorg Med Chem Lett. 2008. PMID: 18255291
1,4-Diazepane compounds as potent and selective CB2 agonists: optimization of metabolic stability.
Riether D, Wu L, Cirillo PF, Berry A, Walker ER, Ermann M, Noya-Marino B, Jenkins JE, Albaugh D, Albrecht C, Fisher M, Gemkow MJ, Grbic H, Löbbe S, Möller C, O'Shea K, Sauer A, Shih DT, Thomson DS. Riether D, et al. Among authors: ermann m. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2011-6. doi: 10.1016/j.bmcl.2011.02.017. Epub 2011 Feb 25. Bioorg Med Chem Lett. 2011. PMID: 21354795
Selective CB2 receptor agonists. Part 2: Structure-activity relationship studies and optimization of proline-based compounds.
Riether D, Zindell R, Wu L, Betageri R, Jenkins JE, Khor S, Berry AK, Hickey ER, Ermann M, Albrecht C, Ceci A, Gemkow MJ, Nagaraja NV, Romig H, Sauer A, Thomson DS. Riether D, et al. Among authors: ermann m. Bioorg Med Chem Lett. 2015 Feb 1;25(3):581-6. doi: 10.1016/j.bmcl.2014.12.019. Epub 2014 Dec 13. Bioorg Med Chem Lett. 2015. PMID: 25556092
Novel 2-aminopyrimidine carbamates as potent and orally active inhibitors of Lck: synthesis, SAR, and in vivo antiinflammatory activity.
Martin MW, Newcomb J, Nunes JJ, McGowan DC, Armistead DM, Boucher C, Buchanan JL, Buckner W, Chai L, Elbaum D, Epstein LF, Faust T, Flynn S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Lee JH, Metz D, Middleton S, Mohn D, Morgenstern K, Morrison MJ, Novak PM, Oliveira-dos-Santos A, Powers D, Rose P, Schneider S, Sell S, Tudor Y, Turci SM, Welcher AA, White RD, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Amouzegh P, Ermann M, Jenkins J, Johnston D, Napier S, Power E. Martin MW, et al. Among authors: ermann m. J Med Chem. 2006 Aug 10;49(16):4981-91. doi: 10.1021/jm060435i. J Med Chem. 2006. PMID: 16884310
Structure-based design of novel 2-amino-6-phenyl-pyrimido[5',4':5,6]pyrimido[1,2-a]benzimidazol-5(6H)-ones as potent and orally active inhibitors of lymphocyte specific kinase (Lck): synthesis, SAR, and in vivo anti-inflammatory activity.
Martin MW, Newcomb J, Nunes JJ, Boucher C, Chai L, Epstein LF, Faust T, Flores S, Gallant P, Gore A, Gu Y, Hsieh F, Huang X, Kim JL, Middleton S, Morgenstern K, Oliveira-dos-Santos A, Patel VF, Powers D, Rose P, Tudor Y, Turci SM, Welcher AA, Zack D, Zhao H, Zhu L, Zhu X, Ghiron C, Ermann M, Johnston D, Saluste CG. Martin MW, et al. Among authors: ermann m. J Med Chem. 2008 Mar 27;51(6):1637-48. doi: 10.1021/jm701095m. Epub 2008 Feb 16. J Med Chem. 2008. PMID: 18278858
39 results