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t-Butyl pyridine and phenyl C-region analogues of 2-(3-fluoro-4-methylsulfonylaminophenyl)propanamides as potent TRPV1 antagonists.
Lee S, Kang DW, Ryu H, Kim C, Ann J, Lee H, Kim E, Hong S, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Lee S, et al. Among authors: stockhausen h. Bioorg Med Chem. 2017 Apr 15;25(8):2451-2462. doi: 10.1016/j.bmc.2017.03.004. Epub 2017 Mar 6. Bioorg Med Chem. 2017. PMID: 28314510 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: stockhausen h. 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-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: stockhausen h. 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.
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: stockhausen h. 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
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: stockhausen h. 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.
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: stockhausen h. 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.
Structure activity relationships of benzyl C-region analogs of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamides as potent TRPV1 antagonists.
Ann J, Jung A, Kim MY, Kim HM, Ryu H, Kim S, Kang DW, Hong S, Cui M, Choi S, Blumberg PM, Frank-Foltyn R, Bahrenberg G, Stockhausen H, Christoph T, Lee J. Ann J, et al. Among authors: stockhausen h. Bioorg Med Chem. 2015 Nov 1;23(21):6844-54. doi: 10.1016/j.bmc.2015.10.001. Epub 2015 Oct 9. Bioorg Med Chem. 2015. PMID: 26474664 Free PMC article.
40 results