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Page 1
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 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 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
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
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
Pyrazolinone-piperidine dipeptide growth hormone secretagogues (GHSs). Discovery of capromorelin.
Carpino PA, Lefker BA, Toler SM, Pan LC, Hadcock JR, Cook ER, DiBrino JN, Campeta AM, DeNinno SL, Chidsey-Frink KL, Hada WA, Inthavongsay J, Mangano FM, Mullins MA, Nickerson DF, Ng O, Pirie CM, Ragan JA, Rose CR, Tess DA, Wright AS, Yu L, Zawistoski MP, DaSilva-Jardine PA, Wilson TC, Thompson DD. Carpino PA, et al. Bioorg Med Chem. 2003 Feb 20;11(4):581-90. doi: 10.1016/s0968-0896(02)00433-9. Bioorg Med Chem. 2003. PMID: 12538023
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
27 results