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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: carpino pa. 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 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
New bicyclic cannabinoid receptor-1 (CB1-R) antagonists.
Carpino PA, Griffith DA, Sakya S, Dow RL, Black SC, Hadcock JR, Iredale PA, Scott DO, Fichtner MW, Rose CR, Day R, Dibrino J, Butler M, Debartolo DB, Dutcher D, Gautreau D, Lizano JS, O'connor RE, Sands MA, Kelly-Sullivan D, Ward KM. Carpino PA, et al. Bioorg Med Chem Lett. 2006 Feb;16(3):731-6. doi: 10.1016/j.bmcl.2005.10.019. Epub 2005 Nov 2. Bioorg Med Chem Lett. 2006. PMID: 16263283
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. Among authors: carpino pa. 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. Among authors: carpino pa. J Med Chem. 2009 May 14;52(9):2652-5. doi: 10.1021/jm900255t. J Med Chem. 2009. PMID: 19351113
Quantitative in vitro and in vivo pharmacological profile of CE-178253, a potent and selective cannabinoid type 1 (CB1) receptor antagonist.
Hadcock JR, Carpino PA, Iredale PA, Dow RL, Gautreau D, Thiede L, Kelly-Sullivan D, Lizano JS, Liu X, Van Deusen J, Ward KM, O'Connor RE, Black SC, Griffith DA, Scott DO. Hadcock JR, et al. Among authors: carpino pa. BMC Pharmacol. 2010 Aug 16;10:9. doi: 10.1186/1471-2210-10-9. BMC Pharmacol. 2010. PMID: 20712891 Free PMC article.
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
38 results