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Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.
Zhu Z, Sun ZY, Ye Y, Voigt J, Strickland C, Smith EM, Cumming J, Wang L, Wong J, Wang YS, Wyss DF, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Parker E, McKittrick BA, Stamford A, Czarniecki M, Greenlee W, Hunter JC. Zhu Z, et al. Among authors: czarniecki m. J Med Chem. 2010 Feb 11;53(3):951-65. doi: 10.1021/jm901408p. J Med Chem. 2010. PMID: 20043696
Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.
Cumming JN, Smith EM, Wang L, Misiaszek J, Durkin J, Pan J, Iserloh U, Wu Y, Zhu Z, Strickland C, Voigt J, Chen X, Kennedy ME, Kuvelkar R, Hyde LA, Cox K, Favreau L, Czarniecki MF, Greenlee WJ, McKittrick BA, Parker EM, Stamford AW. Cumming JN, et al. Among authors: czarniecki mf. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2444-9. doi: 10.1016/j.bmcl.2012.02.013. Epub 2012 Feb 16. Bioorg Med Chem Lett. 2012. PMID: 22390835
Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists.
Zhu Z, Sun ZY, Ye Y, McKittrick B, Greenlee W, Czarniecki M, Fawzi A, Zhang H, Lachowicz JE. Zhu Z, et al. Among authors: czarniecki m. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5218-21. doi: 10.1016/j.bmcl.2009.07.012. Epub 2009 Jul 9. Bioorg Med Chem Lett. 2009. PMID: 19643610
Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.
Wang YS, Strickland C, Voigt JH, Kennedy ME, Beyer BM, Senior MM, Smith EM, Nechuta TL, Madison VS, Czarniecki M, McKittrick BA, Stamford AW, Parker EM, Hunter JC, Greenlee WJ, Wyss DF. Wang YS, et al. Among authors: czarniecki m. J Med Chem. 2010 Feb 11;53(3):942-50. doi: 10.1021/jm901472u. J Med Chem. 2010. PMID: 20043700
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.
Sun ZY, Asberom T, Bara T, Bennett C, Burnett D, Chu I, Clader J, Cohen-Williams M, Cole D, Czarniecki M, Durkin J, Gallo G, Greenlee W, Josien H, Huang X, Hyde L, Jones N, Kazakevich I, Li H, Liu X, Lee J, Maccoss M, Mandal MB, McCracken T, Nomeir A, Mazzola R, Palani A, Parker EM, Pissarnitski DA, Qin J, Song L, Terracina G, Vicarel M, Voigt J, Xu R, Zhang L, Zhang Q, Zhao Z, Zhu X, Zhu Z. Sun ZY, et al. Among authors: czarniecki m. J Med Chem. 2012 Jan 12;55(1):489-502. doi: 10.1021/jm201407j. Epub 2011 Dec 8. J Med Chem. 2012. PMID: 22098494
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.
McKittrick BA, Caldwell JP, Bara T, Boykow G, Chintala M, Clader J, Czarniecki M, Courneya B, Duffy R, Fleming L, Giessert R, Greenlee WJ, Heap C, Hong L, Huang Y, Iserloh U, Josien H, Khan T, Korfmacher W, Liang X, Mazzola R, Mitra S, Moore K, Orth P, Rajagopalan M, Roy S, Sakwa S, Strickland C, Vaccaro H, Voigt J, Wang H, Wong J, Zhang R, Zych A. McKittrick BA, et al. Among authors: czarniecki m. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1592-6. doi: 10.1016/j.bmcl.2015.02.003. Epub 2015 Feb 10. Bioorg Med Chem Lett. 2015. PMID: 25728416
Discovery and synthesis of a novel series of quinoline-based thrombin receptor (PAR-1) antagonists.
Clasby MC, Chackalamannil S, Czarniecki M, Doller D, Eagen K, Greenlee WJ, Lin Y, Tsai H, Xia Y, Ahn HS, Agans-Fantuzzi J, Boykow G, Chintala M, Foster C, Bryant M, Lau J. Clasby MC, et al. Among authors: czarniecki m. Bioorg Med Chem Lett. 2006 Mar 15;16(6):1544-8. doi: 10.1016/j.bmcl.2005.12.042. Epub 2005 Dec 27. Bioorg Med Chem Lett. 2006. PMID: 16380251
59 results