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Page 1
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: pearce lv. 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
N-(3-acyloxy-2-benzylpropyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues: novel potent and high affinity antagonists and partial antagonists of the vanilloid receptor.
Lee J, Lee J, Kang M, Shin M, Kim JM, Kang SU, Lim JO, Choi HK, Suh YG, Park HG, Oh U, Kim HD, Park YH, Ha HJ, Kim YH, Toth A, Wang Y, Tran R, Pearce LV, Lundberg DJ, Blumberg PM. Lee J, et al. Among authors: pearce lv. J Med Chem. 2003 Jul 3;46(14):3116-26. doi: 10.1021/jm030089u. J Med Chem. 2003. PMID: 12825950
Analysis of structure-activity relationships for the 'B-region' of N-(3-acyloxy-2-benzylpropyl)-N(')-[4-(methylsulfonylamino)benzyl]thiourea analogues as vanilloid receptor antagonists: discovery of an N-hydroxythiourea analogue with potent analgesic activity.
Lee J, Kang SU, Choi HK, Lee J, Lim JO, Kil MJ, Jin MK, Kim KP, Sung JH, Chung SJ, Ha HJ, Kim YH, Pearce LV, Tran R, Lundberg DJ, Wang Y, Toth A, Blumberg PM. Lee J, et al. Among authors: pearce lv. Bioorg Med Chem Lett. 2004 May 3;14(9):2291-7. doi: 10.1016/j.bmcl.2004.02.002. Bioorg Med Chem Lett. 2004. PMID: 15081027
Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Lee J, Jin MK, Kang SU, Kim SY, Lee J, Shin M, Hwang J, Cho S, Choi YS, Choi HK, Kim SE, Suh YG, Lee YS, Kim YH, Ha HJ, Toth A, Pearce LV, Tran R, Szabo T, Welter JD, Lundberg DJ, Wang Y, Lazar J, Pavlyukovets VA, Morgan MA, Blumberg PM. Lee J, et al. Among authors: pearce lv. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4143-50. doi: 10.1016/j.bmcl.2005.06.006. Bioorg Med Chem Lett. 2005. PMID: 15993063
Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.
Lee J, Kang SU, Kil MJ, Shin M, Lim JO, Choi HK, Jin MK, Kim SY, Kim SE, Lee YS, Min KH, Kim YH, Ha HJ, Tran R, Welter JD, Wang Y, Szabo T, Pearce LV, Lundberg DJ, Toth A, Pavlyukovets VA, Morgan MA, Blumberg PM. Lee J, et al. Among authors: pearce lv. Bioorg Med Chem Lett. 2005 Sep 15;15(18):4136-42. doi: 10.1016/j.bmcl.2005.06.009. Bioorg Med Chem Lett. 2005. PMID: 16005215
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: pearce lv. 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
53 results