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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
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
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
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
T-type calcium channel blockers: spiro-piperidine azetidines and azetidinones-optimization, design and synthesis.
Smith EM, Sorota S, Kim HM, McKittrick BA, Nechuta TL, Bennett C, Knutson C, Burnett DA, Kieselgof J, Tan Z, Rindgen D, Bridal T, Zhou X, Jia YP, Dong Z, Mullins D, Zhang X, Priestley T, Correll CC, Tulshian D, Czarniecki M, Greenlee WJ. Smith EM, et al. Among authors: czarniecki m. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4602-6. doi: 10.1016/j.bmcl.2010.06.012. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20580233
59 results