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Page 1
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: caldwell jp. 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
Iminoheterocycles as gamma-secretase modulators.
Caldwell JP, Bennett CE, McCracken TM, Mazzola RD, Bara T, Buevich A, Burnett DA, Chu I, Cohen-Williams M, Josein H, Hyde L, Lee J, McKittrick B, Song L, Terracina G, Voigt J, Zhang L, Zhu Z. Caldwell JP, et al. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5380-4. doi: 10.1016/j.bmcl.2010.07.121. Epub 2010 Aug 1. Bioorg Med Chem Lett. 2010. PMID: 20724152
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW. Mandal M, et al. Among authors: caldwell jp. J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1. J Med Chem. 2012. PMID: 22989333
Discovery of potent iminoheterocycle BACE1 inhibitors.
Caldwell JP, Mazzola RD, Durkin J, Chen J, Chen X, Favreau L, Kennedy M, Kuvelkar R, Lee J, McHugh N, McKittrick B, Orth P, Stamford A, Strickland C, Voigt J, Wang L, Zhang L, Zhang Q, Zhu Z. Caldwell JP, et al. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5455-9. doi: 10.1016/j.bmcl.2014.10.006. Epub 2014 Oct 23. Bioorg Med Chem Lett. 2014. PMID: 25455483
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: caldwell jp. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
Structure and activity relationships of tartrate-based TACE inhibitors.
Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO. Li D, et al. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20638281
Discovery of silyl proline containing HCV NS5A inhibitors with pan-genotype activity: SAR development.
Nair AG, Zeng Q, Selyutin O, Rosenblum SB, Jiang Y, Yang DY, Keertikar K, Zhou G, Dwyer MP, Kim SH, Shankar B, Yu W, Tong L, Chen L, Mazzola R, Caldwell J, Tang H, Allard ML, Buckle RN, Gauuan PJ, Holst CL, Martin GS, Naicker KP, Vellekoop S, Agrawal S, Liu R, Kong R, Ingravallo P, Xia E, Zhai Y, Nomeir A, Kozlowski JA. Nair AG, et al. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1475-9. doi: 10.1016/j.bmcl.2016.01.050. Epub 2016 Jan 19. Bioorg Med Chem Lett. 2016. PMID: 26850003
3H-[1,2,4]-Triazolo[5,1-i]purin-5-amine derivatives as adenosine A2A antagonists.
Silverman LS, Caldwell JP, Greenlee WJ, Kiselgof E, Matasi JJ, Tulshian DB, Arik L, Foster C, Bertorelli R, Monopoli A, Ongini E. Silverman LS, et al. Among authors: caldwell jp. Bioorg Med Chem Lett. 2007 Mar 15;17(6):1659-62. doi: 10.1016/j.bmcl.2006.12.104. Epub 2007 Jan 8. Bioorg Med Chem Lett. 2007. PMID: 17234414
The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety.
Ho GD, Anthes J, Bercovici A, Caldwell JP, Cheng KC, Cui X, Fawzi A, Fernandez X, Greenlee WJ, Hey J, Korfmacher W, Lu SX, McLeod RL, Ng F, Torhan AS, Tan Z, Tulshian D, Varty GB, Xu X, Zhang H. Ho GD, et al. Among authors: caldwell jp. Bioorg Med Chem Lett. 2009 May 1;19(9):2519-23. doi: 10.1016/j.bmcl.2009.03.031. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19339177
Generation of Leads for γ-Secretase Modulation.
Mandal M, Buevich A, Caldwell JP, Hyde L, Huang X, Liu X, McKittrick B, Mazzola RD, Pissarnitski D, Palani A, Zhang L, Parker E, Xiao L, Rindgen D, Zhu Z. Mandal M, et al. Among authors: caldwell jp. J Med Chem. 2020 Aug 13;63(15):8216-8230. doi: 10.1021/acs.jmedchem.0c00446. Epub 2020 Aug 4. J Med Chem. 2020. PMID: 32786237
43 results