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Page 1
Pyridine C-region analogs of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
Ryu H, Seo S, Lee JY, Ha TH, Lee S, Jung A, Ann J, Kim SE, Yoon S, Hong M, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Schiene K, Stockhausen H, Christoph T, Frormann S, Lee J. Ryu H, et al. Among authors: blumberg pm. Eur J Med Chem. 2015 Mar 26;93:101-8. doi: 10.1016/j.ejmech.2015.02.001. Epub 2015 Feb 2. Eur J Med Chem. 2015. PMID: 25659771 Free PMC article.
Alpha-substituted N-(4-tert-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as potent and stereospecific TRPV1 antagonists.
Chung JU, Kim SY, Lim JO, Choi HK, Kang SU, Yoon HS, Ryu H, Kang DW, Lee J, Kang B, Choi S, Toth A, Pearce LV, Pavlyukovets VA, Lundberg DJ, Blumberg PM. Chung JU, et al. Among authors: blumberg pm. Bioorg Med Chem. 2007 Sep 15;15(18):6043-53. doi: 10.1016/j.bmc.2007.06.041. Epub 2007 Jun 26. Bioorg Med Chem. 2007. PMID: 17629487
N-4-t-Butylbenzyl 2-(4-methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the A-region.
Kim YS, Kil MJ, Kang SU, Ryu H, Kim MS, Cho Y, Bhondwe RS, Thorat SA, Sun W, Liu K, Lee JH, Choi S, Pearce LV, Pavlyukovets VA, Morgan MA, Tran R, Lazar J, Blumberg PM, Lee J. Kim YS, et al. Among authors: blumberg pm. Bioorg Med Chem. 2012 Jan 1;20(1):215-24. doi: 10.1016/j.bmc.2011.11.008. Epub 2011 Nov 22. Bioorg Med Chem. 2012. PMID: 22169633 Free PMC article.
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: blumberg pm. 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 transient receptor potential vanilloid 1 (TRPV1) antagonists: structure-activity relationships of 2-amino derivatives in the N-(6-trifluoromethylpyridin-3-ylmethyl) C-region.
Kim MS, Ryu H, Kang DW, Cho SH, Seo S, Park YS, Kim MY, Kwak EJ, Kim YS, Bhondwe RS, Kim HS, Park SG, Son K, Choi S, DeAndrea-Lazarus IA, Pearce LV, Blumberg PM, Frank R, Bahrenberg G, Stockhausen H, Kögel BY, Schiene K, Christoph T, Lee J. Kim MS, et al. Among authors: blumberg pm. J Med Chem. 2012 Oct 11;55(19):8392-408. doi: 10.1021/jm300780p. Epub 2012 Sep 20. J Med Chem. 2012. PMID: 22957803 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: blumberg pm. 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: blumberg pm. 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: blumberg pm. 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.
Asymmetric synthesis and receptor activity of chiral simplified resiniferatoxin (sRTX) analogues as transient receptor potential vanilloid 1 (TRPV1) ligands.
Kim MS, Ki Y, Ahn SY, Yoon S, Kim SE, Park HG, Sun W, Son K, Cui M, Choi S, Pearce LV, Esch TE, Deandrea-Lazarus IA, Blumberg PM, Lee J. Kim MS, et al. Among authors: blumberg pm. Bioorg Med Chem Lett. 2014 Jan 1;24(1):382-5. doi: 10.1016/j.bmcl.2013.10.064. Epub 2013 Nov 6. Bioorg Med Chem Lett. 2014. PMID: 24321344 Free PMC article.
451 results