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Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.
Scanio MJC, Searle XB, Liu B, Koenig JR, Altenbach RJ, Gfesser GA, Bogdan A, Greszler S, Zhao G, Singh A, Fan Y, Swensen AM, Vortherms T, Manelli A, Balut C, Gao W, Yong H, Schrimpf M, Tse C, Kym P, Wang X. Scanio MJC, et al. Among authors: gfesser ga. Bioorg Med Chem Lett. 2022 Sep 15;72:128843. doi: 10.1016/j.bmcl.2022.128843. Epub 2022 Jun 7. Bioorg Med Chem Lett. 2022. PMID: 35688367
Discovery of ABBV/GLPG-3221, a Potent Corrector of CFTR for the Treatment of Cystic Fibrosis.
Scanio MJC, Searle XB, Liu B, Koenig JR, Altenbach R, Gfesser GA, Bogdan A, Greszler S, Zhao G, Singh A, Fan Y, Swensen AM, Vortherms T, Manelli A, Balut C, Jia Y, Gao W, Yong H, Schrimpf M, Tse C, Kym P, Wang X. Scanio MJC, et al. Among authors: gfesser ga. ACS Med Chem Lett. 2019 Oct 31;10(11):1543-1548. doi: 10.1021/acsmedchemlett.9b00377. eCollection 2019 Nov 14. ACS Med Chem Lett. 2019. PMID: 31749908 Free PMC article.
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists.
Gomtsyan A, Schmidt RG, Bayburt EK, Gfesser GA, Voight EA, Daanen JF, Schmidt DL, Cowart MD, Liu H, Altenbach RJ, Kort ME, Clapham B, Cox PB, Shrestha A, Henry R, Whittern DN, Reilly RM, Puttfarcken PS, Brederson JD, Song P, Li B, Huang SM, McDonald HA, Neelands TR, McGaraughty SP, Gauvin DM, Joshi SK, Banfor PN, Segreti JA, Shebley M, Faltynek CR, Dart MJ, Kym PR. Gomtsyan A, et al. Among authors: gfesser ga. J Med Chem. 2016 May 26;59(10):4926-47. doi: 10.1021/acs.jmedchem.6b00287. Epub 2016 May 2. J Med Chem. 2016. PMID: 27077528
Adenosine kinase inhibitors: polar 7-substitutent of pyridopyrimidine derivatives improving their locomotor selectivity.
Zheng GZ, Mao Y, Lee CH, Pratt JK, Koenig JR, Perner RJ, Cowart MD, Gfesser GA, McGaraughty S, Chu KL, Zhu C, Yu H, Kohlhaas K, Alexander KM, Wismer CT, Mikusa J, Jarvis MF, Kowaluk EA, Stewart AO. Zheng GZ, et al. Among authors: gfesser ga. Bioorg Med Chem Lett. 2003 Sep 15;13(18):3041-4. doi: 10.1016/s0960-894x(03)00642-5. Bioorg Med Chem Lett. 2003. PMID: 12941329
5-(3-Bromophenyl)-7-(6-morpholin-4-ylpyridin-3-yl)pyrido[2,3-d]pyrimidin-4-ylamine: structure-activity relationships of 7-substituted heteroaryl analogs as non-nucleoside adenosine kinase inhibitors.
Matulenko MA, Lee CH, Jiang M, Frey RR, Cowart MD, Bayburt EK, Didomenico S, Gfesser GA, Gomtsyan A, Zheng GZ, McKie JA, Stewart AO, Yu H, Kohlhaas KL, Alexander KM, McGaraughty S, Wismer CT, Mikusa J, Marsh KC, Snyder RD, Diehl MS, Kowaluk EA, Jarvis MF, Bhagwat SS. Matulenko MA, et al. Among authors: gfesser ga. Bioorg Med Chem. 2005 Jun 1;13(11):3705-20. doi: 10.1016/j.bmc.2005.03.023. Bioorg Med Chem. 2005. PMID: 15863000
19 results