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2-Alkyl/alkenyl substituted pyridine C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as highly potent TRPV1 antagonists.
Ryu H, Seo S, Cho SH, Kim HS, Jung A, Kang DW, Son K, Cui M, Hong SH, Sharma PK, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Schiene K, Christoph T, Frormann S, Lee J. Ryu H, et al. Among authors: kim hs. Bioorg Med Chem Lett. 2014 Aug 15;24(16):4039-43. doi: 10.1016/j.bmcl.2014.05.074. Epub 2014 Jun 2. Bioorg Med Chem Lett. 2014. PMID: 24948568 Free PMC article.
2-(4-Methylsulfonylaminophenyl) propanamide TRPV1 antagonists: Structure-activity relationships in the B and C-regions.
Sun W, Liu K, Ryu H, Kang DW, Kim YS, Kim MS, Cho Y, Bhondwe RS, Thorat SA, Kim HS, Pearce LV, Pavlyukovets VA, Tran R, Morgan MA, Lazar J, Ryder CB, Toth A, Blumberg PM, Lee J. Sun W, et al. Among authors: kim ms, kim ys, kim hs. Bioorg Med Chem. 2012 Feb 1;20(3):1310-8. doi: 10.1016/j.bmc.2011.12.014. Epub 2011 Dec 23. Bioorg Med Chem. 2012. PMID: 22227463 Free PMC article.
Structure-activity relationships and molecular modeling of the N-(3-pivaloyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl] thiourea template for TRPV1 antagonism.
Bhondwe RS, Kang DW, Kim MS, Kim HS, Park SG, Son K, Choi S, Kuhs KA, Pavlyukovets VA, Pearce LV, Blumberg PM, Lee J. Bhondwe RS, et al. Among authors: kim ms, kim hs. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3656-60. doi: 10.1016/j.bmcl.2012.04.034. Epub 2012 Apr 13. Bioorg Med Chem Lett. 2012. PMID: 22546668 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: kim ms, kim hs. 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: kim ys, kim hs, kim my. 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: kim se, kim ms, kim hs. 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.
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: kim se, kim hs. 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: kim ms, kim hs, kim my. 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.
α-Substituted 2-(3-fluoro-4-methylsulfonamidophenyl)acetamides as potent TRPV1 antagonists.
Tran PT, Kim HS, Ann J, Kim SE, Kim C, Hong M, Hoang VH, Ngo VT, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Tran PT, et al. Among authors: kim se, kim c, kim hs. Bioorg Med Chem Lett. 2015 Jun 1;25(11):2326-30. doi: 10.1016/j.bmcl.2015.04.024. Epub 2015 Apr 12. Bioorg Med Chem Lett. 2015. PMID: 25937016 Free PMC article.
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