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Discovery of Benzopyridone-Based Transient Receptor Potential Vanilloid 1 Agonists and Antagonists and the Structural Elucidation of Their Activity Shift.
Thorat SA, Lee Y, Jung A, Ann J, Ahn S, Baek J, Zuo D, Do N, Jeong JJ, Blumberg PM, Esch TE, Turcios NA, Pearce LV, Ha HJ, Yoo YD, Hong S, Choi S, Lee J. Thorat SA, et al. Among authors: ann j. J Med Chem. 2021 Jan 14;64(1):370-384. doi: 10.1021/acs.jmedchem.0c00982. Epub 2021 Jan 1. J Med Chem. 2021. PMID: 33385210
The SAR analysis of TRPV1 agonists with the α-methylated B-region.
Cho Y, Kim MS, Kim HS, Ann J, Lee J, Pearce LV, Pavlyukovets VA, Morgan MA, Blumberg PM, Lee J. Cho Y, et al. Among authors: ann j. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5227-31. doi: 10.1016/j.bmcl.2012.06.059. Epub 2012 Jun 23. Bioorg Med Chem Lett. 2012. PMID: 22796184 Free PMC article.
2-(3-Fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists: structure activity relationships of the 2-oxy pyridine C-region.
Thorat SA, Kang DW, Ryu H, Kim MS, Kim HS, Ann J, Ha T, Kim SE, Son K, Choi S, Blumberg PM, Frank R, Bahrenberg G, Schiene K, Christoph T, Lee J. Thorat SA, et al. Among authors: ann j. Eur J Med Chem. 2013 Jun;64:589-602. doi: 10.1016/j.ejmech.2013.04.003. Epub 2013 Apr 11. Eur J Med Chem. 2013. PMID: 23685943 Free PMC article.
The carbonate analogues of 5'-halogenated resiniferatoxin as TRPV1 ligands.
Lim KS, Lee H, Kim SE, Ha TH, Ann J, Son K, Choi S, Sun W, Pearce LV, DeAndrea-Lazarus IA, Blumberg PM, Lee J. Lim KS, et al. Among authors: ann j. Eur J Med Chem. 2013 Oct;68:233-43. doi: 10.1016/j.ejmech.2013.07.042. Epub 2013 Aug 9. Eur J Med Chem. 2013. PMID: 23981530 Free PMC article.
TRPV1 antagonist with high analgesic efficacy: 2-Thio pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides.
Ha TH, Ryu H, Kim SE, Kim HS, Ann J, Tran PT, Hoang VH, Son K, Cui M, Choi S, Blumberg PM, Frank R, Bahrenberg G, Schiene K, Christoph T, Frormann S, Lee J. Ha TH, et al. Among authors: ann j. Bioorg Med Chem. 2013 Nov 1;21(21):6657-64. doi: 10.1016/j.bmc.2013.08.015. Epub 2013 Aug 13. Bioorg Med Chem. 2013. PMID: 24035514 Free PMC article.
2-Aryl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.
Ryu H, Seo S, Kim MS, Kim MY, Kim HS, Ann J, Tran PT, Hoang VH, Byun J, Cui M, Son K, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Koegel BY, Christoph T, Frormann S, Lee J. Ryu H, et al. Among authors: ann j. Bioorg Med Chem Lett. 2014 Aug 15;24(16):4044-7. doi: 10.1016/j.bmcl.2014.05.072. Epub 2014 Jun 2. Bioorg Med Chem Lett. 2014. PMID: 25011915 Free PMC article.
6,6-Fused heterocyclic ureas as highly potent TRPV1 antagonists.
Sun W, Kim HS, Lee S, Jung A, Kim SE, Ann J, Yoon S, Choi S, Lee JH, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Schiene K, Stockhausen H, Christoph T, Frormann S, Lee J. Sun W, et al. Among authors: ann j. Bioorg Med Chem Lett. 2015 Feb 15;25(4):803-6. doi: 10.1016/j.bmcl.2014.12.086. Epub 2015 Jan 5. Bioorg Med Chem Lett. 2015. PMID: 25597011
95 results