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Page 1
Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus.
Pfefferkorn JA, Guzman-Perez A, Litchfield J, Aiello R, Treadway JL, Pettersen J, Minich ML, Filipski KJ, Jones CS, Tu M, Aspnes G, Risley H, Bian J, Stevens BD, Bourassa P, D'Aquila T, Baker L, Barucci N, Robertson AS, Bourbonais F, Derksen DR, Macdougall M, Cabrera O, Chen J, Lapworth AL, Landro JA, Zavadoski WJ, Atkinson K, Haddish-Berhane N, Tan B, Yao L, Kosa RE, Varma MV, Feng B, Duignan DB, El-Kattan A, Murdande S, Liu S, Ammirati M, Knafels J, Dasilva-Jardine P, Sweet L, Liras S, Rolph TP. Pfefferkorn JA, et al. Among authors: dasilva jardine p. J Med Chem. 2012 Feb 9;55(3):1318-33. doi: 10.1021/jm2014887. Epub 2012 Jan 24. J Med Chem. 2012. PMID: 22196621
Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1.
Dow RL, Li JC, Pence MP, Gibbs EM, LaPerle JL, Litchfield J, Piotrowski DW, Munchhof MJ, Manion TB, Zavadoski WJ, Walker GS, McPherson RK, Tapley S, Sugarman E, Guzman-Perez A, DaSilva-Jardine P. Dow RL, et al. Among authors: dasilva jardine p. ACS Med Chem Lett. 2011 Mar 18;2(5):407-12. doi: 10.1021/ml200051p. eCollection 2011 May 12. ACS Med Chem Lett. 2011. PMID: 24900321 Free PMC article.
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.
Dow RL, Schneider SR, Paight ES, Hank RF, Chiang P, Cornelius P, Lee E, Newsome WP, Swick AG, Spitzer J, Hargrove DM, Patterson TA, Pandit J, Chrunyk BA, LeMotte PK, Danley DE, Rosner MH, Ammirati MJ, Simons SP, Schulte GK, Tate BF, DaSilva-Jardine P. Dow RL, et al. Bioorg Med Chem Lett. 2003 Feb 10;13(3):379-82. doi: 10.1016/s0960-894x(02)00947-2. Bioorg Med Chem Lett. 2003. PMID: 12565933
Discovery and biological characterization of capromorelin analogues with extended half-lives.
Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Murray MC, Cook ER, DiBrino JN, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Lewis SK, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, Pettersen JC, DaSilva-Jardine PA, Wilson TC, Thompson DD. Carpino PA, et al. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3279-82. doi: 10.1016/s0960-894x(02)00734-5. Bioorg Med Chem Lett. 2002. PMID: 12392732
In vitro and in vivo characterization of 3-[2-[6-(2-tert-butoxyethoxy)pyridin-3-yl]-1H-imidazol-4-yl]benzonitrile hydrochloride salt, a potent and selective NPY5 receptor antagonist.
Elliott RL, Oliver RM, Hammond M, Patterson TA, She L, Hargrove DM, Martin KA, Maurer TS, Kalvass JC, Morgan BP, DaSilva-Jardine PA, Stevenson RW, Mack CM, Cassella JV. Elliott RL, et al. J Med Chem. 2003 Feb 27;46(5):670-3. doi: 10.1021/jm025584p. J Med Chem. 2003. PMID: 12593645
Discovery of 2-(2-chlorophenyl)-3-(4-chlorophenyl)-7-(2,2-difluoropropyl)-6,7-dihydro-2H-pyrazolo[3,4-f][1,4]oxazepin-8(5H)-one (PF-514273), a novel, bicyclic lactam-based cannabinoid-1 receptor antagonist for the treatment of obesity.
Dow RL, Carpino PA, Hadcock JR, Black SC, Iredale PA, DaSilva-Jardine P, Schneider SR, Paight ES, Griffith DA, Scott DO, O'Connor RE, Nduaka CI. Dow RL, et al. J Med Chem. 2009 May 14;52(9):2652-5. doi: 10.1021/jm900255t. J Med Chem. 2009. PMID: 19351113
Bioisosteric replacement of the hydrazide pharmacophore of the cannabinoid-1 receptor antagonist SR141716A. Part I: potent, orally-active 1,4-disubstituted imidazoles.
Dow RL, Hadcock JR, Scott DO, Schneider SR, Paight ES, Iredale PA, Carpino PA, Griffith DA, Hammond M, Dasilva-Jardine P. Dow RL, et al. Among authors: dasilva jardine p. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5351-4. doi: 10.1016/j.bmcl.2009.07.130. Epub 2009 Aug 6. Bioorg Med Chem Lett. 2009. PMID: 19683918
Discovery of 1-[9-(4-chlorophenyl)-8-(2-chlorophenyl)-9H-purin-6-yl]-4-ethylaminopiperidine-4-carboxylic acid amide hydrochloride (CP-945,598), a novel, potent, and selective cannabinoid type 1 receptor antagonist.
Griffith DA, Hadcock JR, Black SC, Iredale PA, Carpino PA, DaSilva-Jardine P, Day R, DiBrino J, Dow RL, Landis MS, O'Connor RE, Scott DO. Griffith DA, et al. J Med Chem. 2009 Jan 22;52(2):234-7. doi: 10.1021/jm8012932. J Med Chem. 2009. PMID: 19102698
Estrogen receptor beta selective ligands: discovery and SAR of novel heterocyclic ligands.
Chesworth R, Wessel MD, Heyden L, Mangano FM, Zawistoski M, Gegnas L, Galluzzo D, Lefker B, Cameron KO, Tickner J, Lu B, Castleberry TA, Petersen DN, Brault A, Perry P, Ng O, Owen TA, Pan L, Ke HZ, Brown TA, Thompson DD, DaSilva-Jardine P. Chesworth R, et al. Bioorg Med Chem Lett. 2005 Dec 15;15(24):5562-6. doi: 10.1016/j.bmcl.2005.08.010. Epub 2005 Oct 10. Bioorg Med Chem Lett. 2005. PMID: 16219463
Liver-Targeted Small-Molecule Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9 Synthesis.
McClure KF, Piotrowski DW, Petersen D, Wei L, Xiao J, Londregan AT, Kamlet AS, Dechert-Schmitt AM, Raymer B, Ruggeri RB, Canterbury D, Limberakis C, Liras S, DaSilva-Jardine P, Dullea RG, Loria PM, Reidich B, Salatto CT, Eng H, Kimoto E, Atkinson K, King-Ahmad A, Scott D, Beaumont K, Chabot JR, Bolt MW, Maresca K, Dahl K, Arakawa R, Takano A, Halldin C. McClure KF, et al. Among authors: dasilva jardine p. Angew Chem Int Ed Engl. 2017 Dec 18;56(51):16218-16222. doi: 10.1002/anie.201708744. Epub 2017 Nov 24. Angew Chem Int Ed Engl. 2017. PMID: 29073340
27 results