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Page 1
A Small-Molecule Oral Agonist of the Human Glucagon-like Peptide-1 Receptor.
Griffith DA, Edmonds DJ, Fortin JP, Kalgutkar AS, Kuzmiski JB, Loria PM, Saxena AR, Bagley SW, Buckeridge C, Curto JM, Derksen DR, Dias JM, Griffor MC, Han S, Jackson VM, Landis MS, Lettiere D, Limberakis C, Liu Y, Mathiowetz AM, Patel JC, Piotrowski DW, Price DA, Ruggeri RB, Tess DA. Griffith DA, et al. J Med Chem. 2022 Jun 23;65(12):8208-8226. doi: 10.1021/acs.jmedchem.1c01856. Epub 2022 Jun 1. J Med Chem. 2022. PMID: 35647711 Free PMC article.
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. Among authors: griffith da. 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. 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: griffith da. J Med Chem. 2009 May 14;52(9):2652-5. doi: 10.1021/jm900255t. J Med Chem. 2009. PMID: 19351113
Short-acting 5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3H)-one derivatives as orally-active calcium-sensing receptor antagonists.
Didiuk MT, Griffith DA, Benbow JW, Liu KK, Walker DP, Bi FC, Morris J, Guzman-Perez A, Gao H, Bechle BM, Kelley RM, Yang X, Dirico K, Ahmed S, Hungerford W, DiBrinno J, Zawistoski MP, Bagley SW, Li J, Zeng Y, Santucci S, Oliver R, Corbett M, Olson T, Chen C, Li M, Paralkar VM, Riccardi KA, Healy DR, Kalgutkar AS, Maurer TS, Nguyen HT, Frederick KS. Didiuk MT, et al. Among authors: griffith da. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4555-9. doi: 10.1016/j.bmcl.2009.07.004. Epub 2009 Jul 8. Bioorg Med Chem Lett. 2009. PMID: 19625189
Discovery tactics to mitigate toxicity risks due to reactive metabolite formation with 2-(2-hydroxyaryl)-5-(trifluoromethyl)pyrido[4,3-d]pyrimidin-4(3h)-one derivatives, potent calcium-sensing receptor antagonists and clinical candidate(s) for the treatment of osteoporosis.
Kalgutkar AS, Griffith DA, Ryder T, Sun H, Miao Z, Bauman JN, Didiuk MT, Frederick KS, Zhao SX, Prakash C, Soglia JR, Bagley SW, Bechle BM, Kelley RM, Dirico K, Zawistoski M, Li J, Oliver R, Guzman-Perez A, Liu KK, Walker DP, Benbow JW, Morris J. Kalgutkar AS, et al. Among authors: griffith da. Chem Res Toxicol. 2010 Jun 21;23(6):1115-26. doi: 10.1021/tx100137n. Chem Res Toxicol. 2010. PMID: 20507089
Synthesis of spiropiperidine lactam acetyl-CoA carboxylase inhibitors.
Huard K, Bagley SW, Menhaji-Klotz E, Préville C, Southers JA Jr, Smith AC, Edmonds DJ, Lucas JC, Dunn MF, Allanson NM, Blaney EL, Garcia-Irizarry CN, Kohrt JT, Griffith DA, Dow RL. Huard K, et al. Among authors: griffith da. J Org Chem. 2012 Nov 16;77(22):10050-7. doi: 10.1021/jo3014808. Epub 2012 Nov 5. J Org Chem. 2012. PMID: 23127254
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.
Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS, Griffith DA, Griffor MC, Guimarães CR, Guzman-Perez A, Han S, Kalgutkar AS, Klug-McLeod J, Garcia-Irizarry C, Li J, Lippa B, Price DA, Southers JA, Walker DP, Wei L, Xiao J, Zawistoski MP, Zhao X. Bhattacharya SK, et al. Among authors: griffith da. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7523-9. doi: 10.1016/j.bmcl.2012.10.039. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23153798
Demonstration of the innate electrophilicity of 4-(3-(benzyloxy)phenyl)-2-(ethylsulfinyl)-6-(trifluoromethyl)pyrimidine (BETP), a small-molecule positive allosteric modulator of the glucagon-like peptide-1 receptor.
Eng H, Sharma R, McDonald TS, Edmonds DJ, Fortin JP, Li X, Stevens BD, Griffith DA, Limberakis C, Nolte WM, Price DA, Jackson M, Kalgutkar AS. Eng H, et al. Among authors: griffith da. Drug Metab Dispos. 2013 Aug;41(8):1470-9. doi: 10.1124/dmd.113.052183. Epub 2013 May 7. Drug Metab Dispos. 2013. PMID: 23653442
88 results