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Page 1
Discovery of 6-ethyl-2,4-diaminopyrimidine-based small molecule renin inhibitors.
Holsworth DD, Jalaie M, Belliotti T, Cai C, Collard W, Ferreira S, Powell NA, Stier M, Zhang E, McConnell P, Mochalkin I, Ryan MJ, Bryant J, Li T, Kasani A, Subedi R, Maiti SN, Edmunds JJ. Holsworth DD, et al. Among authors: mcconnell p. Bioorg Med Chem Lett. 2007 Jul 1;17(13):3575-80. doi: 10.1016/j.bmcl.2007.04.052. Epub 2007 Apr 25. Bioorg Med Chem Lett. 2007. PMID: 17482464
Ketopiperazine-based renin inhibitors: optimization of the "C" ring.
Holsworth DD, Cai C, Cheng XM, Cody WL, Downing DM, Erasga N, Lee C, Powell NA, Edmunds JJ, Stier M, Jalaie M, Zhang E, McConnell P, Ryan MJ, Bryant J, Li T, Kasani A, Hall E, Subedi R, Rahim M, Maiti S. Holsworth DD, et al. Among authors: mcconnell p. Bioorg Med Chem Lett. 2006 May 1;16(9):2500-4. doi: 10.1016/j.bmcl.2006.01.084. Epub 2006 Feb 15. Bioorg Med Chem Lett. 2006. PMID: 16480874
Rational design of 6-(2,4-diaminopyrimidinyl)-1,4-benzoxazin-3-ones as small molecule renin inhibitors.
Powell NA, Ciske FL, Cai C, Holsworth DD, Mennen K, Van Huis CA, Jalaie M, Day J, Mastronardi M, McConnell P, Mochalkin I, Zhang E, Ryan MJ, Bryant J, Collard W, Ferreira S, Gu C, Collins R, Edmunds JJ. Powell NA, et al. Among authors: mcconnell p. Bioorg Med Chem. 2007 Sep 1;15(17):5912-49. doi: 10.1016/j.bmc.2007.05.069. Epub 2007 Jun 2. Bioorg Med Chem. 2007. PMID: 17574423
Novel and selective spiroindoline-based inhibitors of Sky kinase.
Powell NA, Kohrt JT, Filipski KJ, Kaufman M, Sheehan D, Edmunds JE, Delaney A, Wang Y, Bourbonais F, Lee DY, Schwende F, Sun F, McConnell P, Catana C, Chen H, Ohren J, Perrin LA. Powell NA, et al. Among authors: mcconnell p. Bioorg Med Chem Lett. 2012 Jan 1;22(1):190-3. doi: 10.1016/j.bmcl.2011.11.036. Epub 2011 Nov 16. Bioorg Med Chem Lett. 2012. PMID: 22119469
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.
Sarver RW, Peevers J, Cody WL, Ciske FL, Dyer J, Emerson SD, Hagadorn JC, Holsworth DD, Jalaie M, Kaufman M, Mastronardi M, McConnell P, Powell NA, Quin J 3rd, Van Huis CA, Zhang E, Mochalkin I. Sarver RW, et al. Among authors: mcconnell p. Anal Biochem. 2007 Jan 1;360(1):30-40. doi: 10.1016/j.ab.2006.10.017. Epub 2006 Oct 30. Anal Biochem. 2007. PMID: 17113558
Highly selective 2,4-diaminopyrimidine-5-carboxamide inhibitors of Sky kinase.
Powell NA, Hoffman JK, Ciske FL, Kaufman MD, Kohrt JT, Quin J 3rd, Sheehan DJ, Delaney A, Baxi SM, Catana C, McConnell P, Ohren J, Perrin LA, Edmunds JJ. Powell NA, et al. Among authors: mcconnell p. Bioorg Med Chem Lett. 2013 Feb 15;23(4):1046-50. doi: 10.1016/j.bmcl.2012.12.013. Epub 2012 Dec 20. Bioorg Med Chem Lett. 2013. PMID: 23312472
Effects of modifications of the linker in a series of phenylpropanoic acid derivatives: Synthesis, evaluation as PPARalpha/gamma dual agonists, and X-ray crystallographic studies.
Casimiro-Garcia A, Bigge CF, Davis JA, Padalino T, Pulaski J, Ohren JF, McConnell P, Kane CD, Royer LJ, Stevens KA, Auerbach BJ, Collard WT, McGregor C, Fakhoury SA, Schaum RP, Zhou H. Casimiro-Garcia A, et al. Among authors: mcconnell p. Bioorg Med Chem. 2008 May 1;16(9):4883-907. doi: 10.1016/j.bmc.2008.03.043. Epub 2008 Mar 20. Bioorg Med Chem. 2008. PMID: 18394907
Synthesis and evaluation of novel alpha-heteroaryl-phenylpropanoic acid derivatives as PPARalpha/gamma dual agonists.
Casimiro-Garcia A, Bigge CF, Davis JA, Padalino T, Pulaski J, Ohren JF, McConnell P, Kane CD, Royer LJ, Stevens KA, Auerbach B, Collard W, McGregor C, Song K. Casimiro-Garcia A, et al. Among authors: mcconnell p. Bioorg Med Chem. 2009 Oct 15;17(20):7113-25. doi: 10.1016/j.bmc.2009.09.001. Epub 2009 Sep 6. Bioorg Med Chem. 2009. PMID: 19783444
Discovery of a series of 2-(1H-pyrazol-1-yl)pyridines as ALK5 inhibitors with potential utility in the prevention of dermal scarring.
Boys ML, Bian F, Kramer JB, Chio CL, Ren XD, Chen H, Barrett SD, Sexton KE, Iula DM, Filzen GF, Nguyen MN, Angell P, Downs VL, Wang Z, Raheja N, Ellsworth EL, Fakhoury S, Bratton LD, Keller PR, Gowan R, Drummond EM, Maiti SN, Hena MA, Lu L, McConnell P, Knafels JD, Thanabal V, Sun F, Alessi D, McCarthy A, Zhang E, Finzel BC, Patel S, Ciotti SM, Eisma R, Payne NA, Gilbertsen RB, Kostlan CR, Pocalyko DJ, Lala DS. Boys ML, et al. Among authors: mcconnell p. Bioorg Med Chem Lett. 2012 May 15;22(10):3392-7. doi: 10.1016/j.bmcl.2012.04.013. Epub 2012 Apr 10. Bioorg Med Chem Lett. 2012. PMID: 22542194
The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases.
Hu LY, Boxer PA, Kesten SR, Lei HJ, Wustrow DJ, Moreland DW, Zhang L, Ahn K, Ryder TR, Liu X, Rubin JR, Fahnoe K, Carroll RT, Dutta S, Fahnoe DC, Probert AW, Roof RL, Rafferty MF, Kostlan CR, Scholten JD, Hood M, Ren XD, Schielke GP, Su TZ, Taylor CP, Mistry A, McConnell P, Hasemann C, Ohren J. Hu LY, et al. Among authors: mcconnell p. Bioorg Med Chem Lett. 2006 May 1;16(9):2337-40. doi: 10.1016/j.bmcl.2005.07.058. Epub 2005 Sep 6. Bioorg Med Chem Lett. 2006. PMID: 16143519
189 results