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Page 1
cis-2,5-dicyanopyrrolidine inhibitors of dipeptidyl peptidase IV: synthesis and in vitro, in vivo, and X-ray crystallographic characterization.
Wright SW, Ammirati MJ, Andrews KM, Brodeur AM, Danley DE, Doran SD, Lillquist JS, McClure LD, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soeller WC, Soglia CB, Treadway JL, VanVolkenburg MA, Wang H, Wilder DC, Olson TV. Wright SW, et al. Among authors: polivkova j. J Med Chem. 2006 Jun 1;49(11):3068-76. doi: 10.1021/jm0600085. J Med Chem. 2006. PMID: 16722626
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone: a potent, selective, orally active dipeptidyl peptidase IV inhibitor.
Ammirati MJ, Andrews KM, Boyer DD, Brodeur AM, Danley DE, Doran SD, Hulin B, Liu S, McPherson RK, Orena SJ, Parker JC, Polivkova J, Qiu X, Soglia CB, Treadway JL, VanVolkenburg MA, Wilder DC, Piotrowski DW. Ammirati MJ, et al. Among authors: polivkova j. Bioorg Med Chem Lett. 2009 Apr 1;19(7):1991-5. doi: 10.1016/j.bmcl.2009.02.041. Epub 2009 Feb 13. Bioorg Med Chem Lett. 2009. PMID: 19275964
Discovery of new piperidine amide triazolobenzodiazepinones as intestinal-selective CCK1 receptor agonists.
Cameron KO, Beretta EE, Chen Y, Chu-Moyer M, Fernando D, Gao H, Kohrt J, Lavergne S, Jardine Pda S, Guzman-Perez A, Hoth C, Perry DA, Hadcock JR, Gautreau D, Makowski M, Perez S, Polivkova J, Rogers L, Scott DO, Swick AG, Thiede L, Trebino CE, Trilles RV, Wilmowski J, Zhang Y. Cameron KO, et al. Among authors: polivkova j. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2943-7. doi: 10.1016/j.bmcl.2012.02.049. Epub 2012 Feb 23. Bioorg Med Chem Lett. 2012. PMID: 22424974
Spirolactam-based acetyl-CoA carboxylase inhibitors: toward improved metabolic stability of a chromanone lead structure.
Griffith DA, Dow RL, Huard K, Edmonds DJ, Bagley SW, Polivkova J, Zeng D, Garcia-Irizarry CN, Southers JA, Esler W, Amor P, Loomis K, McPherson K, Bahnck KB, Préville C, Banks T, Moore DE, Mathiowetz AM, Menhaji-Klotz E, Smith AC, Doran SD, Beebe DA, Dunn MF. Griffith DA, et al. Among authors: polivkova j. J Med Chem. 2013 Sep 12;56(17):7110-9. doi: 10.1021/jm401033t. Epub 2013 Aug 27. J Med Chem. 2013. PMID: 23981033
Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3.
Huard K, Londregan AT, Tesz G, Bahnck KB, Magee TV, Hepworth D, Polivkova J, Coffey SB, Pabst BA, Gosset JR, Nigam A, Kou K, Sun H, Lee K, Herr M, Boehm M, Carpino PA, Goodwin B, Perreault C, Li Q, Jorgensen CC, Tkalcevic GT, Subashi TA, Ahn K. Huard K, et al. Among authors: polivkova j. J Med Chem. 2015 Sep 24;58(18):7164-72. doi: 10.1021/acs.jmedchem.5b01008. Epub 2015 Sep 8. J Med Chem. 2015. PMID: 26258602
Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family.
Huard K, Gosset JR, Montgomery JI, Gilbert A, Hayward MM, Magee TV, Cabral S, Uccello DP, Bahnck K, Brown J, Purkal J, Gorgoglione M, Lanba A, Futatsugi K, Herr M, Genung NE, Aspnes G, Polivkova J, Garcia-Irizarry CN, Li Q, Canterbury D, Niosi M, Vera NB, Li Z, Khunte B, Siderewicz J, Rolph T, Erion DM. Huard K, et al. Among authors: polivkova j. J Med Chem. 2016 Feb 11;59(3):1165-75. doi: 10.1021/acs.jmedchem.5b01752. Epub 2016 Jan 27. J Med Chem. 2016. PMID: 26734723
Optimization of Metabolic and Renal Clearance in a Series of Indole Acid Direct Activators of 5'-Adenosine Monophosphate-Activated Protein Kinase (AMPK).
Edmonds DJ, Kung DW, Kalgutkar AS, Filipski KJ, Ebner DC, Cabral S, Smith AC, Aspnes GE, Bhattacharya SK, Borzilleri KA, Brown JA, Calabrese MF, Caspers NL, Cokorinos EC, Conn EL, Dowling MS, Eng H, Feng B, Fernando DP, Genung NE, Herr M, Kurumbail RG, Lavergne SY, Lee EC, Li Q, Mathialagan S, Miller RA, Panteleev J, Polivkova J, Rajamohan F, Reyes AR, Salatto CT, Shavnya A, Thuma BA, Tu M, Ward J, Withka JM, Xiao J, Cameron KO. Edmonds DJ, et al. Among authors: polivkova j. J Med Chem. 2018 Mar 22;61(6):2372-2383. doi: 10.1021/acs.jmedchem.7b01641. Epub 2018 Feb 28. J Med Chem. 2018. PMID: 29466005
Optimizing the Benefit/Risk of Acetyl-CoA Carboxylase Inhibitors through Liver Targeting.
Huard K, Smith AC, Cappon G, Dow RL, Edmonds DJ, El-Kattan A, Esler WP, Fernando DP, Griffith DA, Kalgutkar AS, Ross TT, Bagley SW, Beebe D, Bi YA, Cabral S, Crowley C, Doran SD, Dowling MS, Liras S, Mascitti V, Niosi M, Pfefferkorn JA, Polivkova J, Préville C, Price DA, Shavnya A, Shirai N, Smith AH, Southers JR, Tess DA, Thuma BA, Varma MV, Yang X. Huard K, et al. Among authors: polivkova j. J Med Chem. 2020 Oct 8;63(19):10879-10896. doi: 10.1021/acs.jmedchem.0c00640. Epub 2020 Sep 18. J Med Chem. 2020. PMID: 32809824
Small molecule inhibitors of PCSK9. SAR investigations of head and amine groups.
Aspnes GE, Coffey SB, Darout E, Dechert-Schmitt AM, Dullea RG, Kamlet AS, Limberakis C, Londregan AT, McClure KF, Menhaji-Klotz E, Piotrowski DW, Polivkova J, Raymer B, Ruggeri RB, Salatto CT, Tu M, Wei L, Xiao J. Aspnes GE, et al. Among authors: polivkova j. Bioorg Med Chem Lett. 2023 Aug 15;92:129394. doi: 10.1016/j.bmcl.2023.129394. Epub 2023 Jun 26. Bioorg Med Chem Lett. 2023. PMID: 37379958
38 results