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Page 1
Acylguanidines as small-molecule beta-secretase inhibitors.
Cole DC, Manas ES, Stock JR, Condon JS, Jennings LD, Aulabaugh A, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jin G, Lin L, Lovering FE, Malamas MS, Stahl ML, Strand J, Sukhdeo MN, Svenson K, Turner MJ, Wagner E, Wu J, Zhou P, Bard J. Cole DC, et al. Among authors: stock jr. J Med Chem. 2006 Oct 19;49(21):6158-61. doi: 10.1021/jm0607451. J Med Chem. 2006. PMID: 17034121
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE. Cole DC, et al. Among authors: stock jr. J Med Chem. 2007 Nov 15;50(23):5535-8. doi: 10.1021/jm070521y. Epub 2007 Oct 19. J Med Chem. 2007. PMID: 17948978
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Cole DC, Stock JR, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jennings LD, Jin G, Lohse PA, Malamas MS, Manas ES, Moore WJ, O'Donnell MM, Olland AM, Robichaud AJ, Svenson K, Wu J, Wagner E, Bard J. Cole DC, et al. Among authors: stock jr. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1063-6. doi: 10.1016/j.bmcl.2007.12.010. Epub 2007 Dec 10. Bioorg Med Chem Lett. 2008. PMID: 18162398
Identification, characterization and initial hit-to-lead optimization of a series of 4-arylamino-3-pyridinecarbonitrile as protein kinase C theta (PKCtheta) inhibitors.
Cole DC, Asselin M, Brennan A, Czerwinski R, Ellingboe JW, Fitz L, Greco R, Huang X, Joseph-McCarthy D, Kelly MF, Kirisits M, Lee J, Li Y, Morgan P, Stock JR, Tsao DH, Wissner A, Yang X, Chaudhary D. Cole DC, et al. Among authors: stock jr. J Med Chem. 2008 Oct 9;51(19):5958-63. doi: 10.1021/jm800214a. Epub 2008 Sep 11. J Med Chem. 2008. PMID: 18783200
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.
Nowak P, Cole DC, Aulabaugh A, Bard J, Chopra R, Cowling R, Fan KY, Hu B, Jacobsen S, Jani M, Jin G, Lo MC, Malamas MS, Manas ES, Narasimhan R, Reinhart P, Robichaud AJ, Stock JR, Subrath J, Svenson K, Turner J, Wagner E, Zhou P, Ellingboe JW. Nowak P, et al. Among authors: stock jr. Bioorg Med Chem Lett. 2010 Jan 15;20(2):632-5. doi: 10.1016/j.bmcl.2009.11.052. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 19959359
Benzimidazole- and indole-substituted 1,3'-bipyrrolidine benzamides as histamine H3 receptor antagonists.
Cole DC, Gross JL, Comery TA, Aschmies S, Hirst WD, Kelley C, Kim JI, Kubek K, Ning X, Platt BJ, Robichaud AJ, Solvibile WR, Stock JR, Tawa G, Williams MJ, Ellingboe JW. Cole DC, et al. Among authors: stock jr. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1237-40. doi: 10.1016/j.bmcl.2009.11.122. Epub 2009 Dec 4. Bioorg Med Chem Lett. 2010. PMID: 20042333
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.
Jennings LD, Cole DC, Stock JR, Sukhdeo MN, Ellingboe JW, Cowling R, Jin G, Manas ES, Fan KY, Malamas MS, Harrison BL, Jacobsen S, Chopra R, Lohse PA, Moore WJ, O'Donnell MM, Hu Y, Robichaud AJ, Turner MJ, Wagner E, Bard J. Jennings LD, et al. Among authors: stock jr. Bioorg Med Chem Lett. 2008 Jan 15;18(2):767-71. doi: 10.1016/j.bmcl.2007.11.043. Epub 2007 Nov 17. Bioorg Med Chem Lett. 2008. PMID: 18068983
28 results