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Page 1
Rapid Evolution of a Fragment-like Molecule to Pan-Metallo-Beta-Lactamase Inhibitors: Initial Leads toward Clinical Candidates.
Mandal M, Xiao L, Pan W, Scapin G, Li G, Tang H, Yang SW, Pan J, Root Y, de Jesus RK, Yang C, Prosise W, Dayananth P, Mirza A, Therien AG, Young K, Flattery A, Garlisi C, Zhang R, Chu D, Sheth P, Chu I, Wu J, Markgraf C, Kim HY, Painter R, Mayhood TW, DiNunzio E, Wyss DF, Buevich AV, Fischmann T, Pasternak A, Dong S, Hicks JD, Villafania A, Liang L, Murgolo N, Black T, Hagmann WK, Tata J, Parmee ER, Weber AE, Su J, Tang H. Mandal M, et al. Among authors: parmee er. J Med Chem. 2022 Dec 22;65(24):16234-16251. doi: 10.1021/acs.jmedchem.2c00766. Epub 2022 Dec 7. J Med Chem. 2022. PMID: 36475645
Can We Make Small Molecules Lean? Optimization of a Highly Lipophilic TarO Inhibitor.
Mandal M, Tan Z, Madsen-Duggan C, Buevich AV, Caldwell JP, Dejesus R, Flattery A, Garlisi CG, Gill C, Ha SN, Ho G, Koseoglu S, Labroli M, Basu K, Lee SH, Liang L, Liu J, Mayhood T, McGuinness D, McLaren DG, Wen X, Parmee E, Rindgen D, Roemer T, Sheth P, Tawa P, Tata J, Yang C, Yang SW, Xiao L, Wang H, Tan C, Tang H, Walsh P, Walsh E, Wu J, Su J. Mandal M, et al. J Med Chem. 2017 May 11;60(9):3851-3865. doi: 10.1021/acs.jmedchem.7b00113. Epub 2017 Mar 29. J Med Chem. 2017. PMID: 28322556
Discovery of a potent and selective ROMK inhibitor with improved pharmacokinetic properties based on an octahydropyrazino[2,1-c][1,4]oxazine scaffold.
Zhu Y, de Jesus RK, Tang H, Walsh SP, Jiang J, Gu X, Teumelsan N, Shahripour A, Pio B, Ding FX, Ha S, Priest BT, Swensen AM, Alonso-Galicia M, Felix JP, Brochu RM, Bailey T, Thomas-Fowlkes B, Zhou X, Pai LY, Hampton C, Hernandez M, Owens K, Ehrhart J, Roy S, Kaczorowski GJ, Yang L, Parmee ER, Sullivan K, Garcia ML, Pasternak A. Zhu Y, et al. Among authors: parmee er. Bioorg Med Chem Lett. 2016 Dec 1;26(23):5695-5702. doi: 10.1016/j.bmcl.2016.10.064. Epub 2016 Oct 24. Bioorg Med Chem Lett. 2016. PMID: 27839686
Discovery of MK-8153, a Potent and Selective ROMK Inhibitor and Novel Diuretic/Natriuretic.
Jiang J, Ding FX, Zhou X, Bateman TJ, Dong S, Gu X, Keh deJesus R, Pio B, Tang H, Chobanian HR, Levorse D, Hu M, Thomas-Fowlkes B, Margulis M, Koehler M, Weinglass A, Gibson J, Houle K, Yudkovitz J, Hampton C, Pai LY, Samuel K, Cutarelli T, Sullivan K, Parmee ER, Davies I, Pasternak A. Jiang J, et al. Among authors: parmee er. J Med Chem. 2021 Jun 10;64(11):7691-7701. doi: 10.1021/acs.jmedchem.1c00406. Epub 2021 May 26. J Med Chem. 2021. PMID: 34038119
Discovery of potent and selective dipeptidyl peptidase IV inhibitors derived from beta-aminoamides bearing subsituted triazolopiperazines.
Kim D, Kowalchick JE, Brockunier LL, Parmee ER, Eiermann GJ, Fisher MH, He H, Leiting B, Lyons K, Scapin G, Patel SB, Petrov A, Pryor KD, Roy RS, Wu JK, Zhang X, Wyvratt MJ, Zhang BB, Zhu L, Thornberry NA, Weber AE. Kim D, et al. Among authors: parmee er. J Med Chem. 2008 Feb 14;51(3):589-602. doi: 10.1021/jm070330v. Epub 2008 Jan 18. J Med Chem. 2008. PMID: 18201067
Discovery of MK-1454: A Potent Cyclic Dinucleotide Stimulator of Interferon Genes Agonist for the Treatment of Cancer.
Chang W, Altman MD, Lesburg CA, Perera SA, Piesvaux JA, Schroeder GK, Wyss DF, Cemerski S, Chen Y, DiNunzio E, Haidle AM, Ho T, Kariv I, Knemeyer I, Kopinja JE, Lacey BM, Laskey J, Lim J, Long BJ, Ma Y, Maddess ML, Pan BS, Presland JP, Spooner E, Steinhuebel D, Truong Q, Zhang Z, Fu J, Addona GH, Northrup AB, Parmee E, Tata JR, Bennett DJ, Cumming JN, Siu T, Trotter BW. Chang W, et al. J Med Chem. 2022 Apr 14;65(7):5675-5689. doi: 10.1021/acs.jmedchem.1c02197. Epub 2022 Mar 25. J Med Chem. 2022. PMID: 35332774
Substituted piperazines as novel dipeptidyl peptidase IV inhibitors.
Brockunier LL, He J, Colwell LF Jr, Habulihaz B, He H, Leiting B, Lyons KA, Marsilio F, Patel RA, Teffera Y, Wu JK, Thornberry NA, Weber AE, Parmee ER. Brockunier LL, et al. Among authors: parmee er. Bioorg Med Chem Lett. 2004 Sep 20;14(18):4763-6. doi: 10.1016/j.bmcl.2004.06.065. Bioorg Med Chem Lett. 2004. PMID: 15324904
Potent and selective proline derived dipeptidyl peptidase IV inhibitors.
Edmondson SD, Mastracchio A, Beconi M, Colwell LF Jr, Habulihaz B, He H, Kumar S, Leiting B, Lyons KA, Mao A, Marsilio F, Patel RA, Wu JK, Zhu L, Thornberry NA, Weber AE, Parmee ER. Edmondson SD, et al. Among authors: parmee er. Bioorg Med Chem Lett. 2004 Oct 18;14(20):5151-5. doi: 10.1016/j.bmcl.2004.07.056. Bioorg Med Chem Lett. 2004. PMID: 15380217
47 results