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Items: 1 to 20 of 86

1.

Heterocycle-linked phenylbenzyl amides as novel TRPV1 antagonists and their TRPV1 binding modes: constraint-induced enhancement of in vitro and in vivo activities.

Kim NJ, Li FN, Lee JH, Park SG, Kim K, Lim C, Han YT, Yun H, Jung JW, Park HG, Kim HD, Woo BY, Shin SS, Kim SY, Choi JK, Jeong YS, Park Y, Park YH, Kim DD, Choi S, Suh YG.

Chem Asian J. 2013 Feb;8(2):400-9. doi: 10.1002/asia.201200730. Epub 2012 Dec 3.

PMID:
23208797
2.

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.

Bioorg Med Chem. 2013 Nov 1;21(21):6657-64. doi: 10.1016/j.bmc.2013.08.015. Epub 2013 Aug 13.

PMID:
24035514
3.

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.

Bioorg Med Chem. 2015 Nov 1;23(21):6844-54. doi: 10.1016/j.bmc.2015.10.001. Epub 2015 Oct 9.

PMID:
26474664
4.

Discovery of novel 5,5-diarylpentadienamides as orally available transient receptor potential vanilloid 1 (TRPV1) antagonists.

Saku O, Ishida H, Atsumi E, Sugimoto Y, Kodaira H, Kato Y, Shirakura S, Nakasato Y.

J Med Chem. 2012 Apr 12;55(7):3436-51. doi: 10.1021/jm300101n. Epub 2012 Mar 22.

PMID:
22394104
5.

Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.

Wang HL, Katon J, Balan C, Bannon AW, Bernard C, Doherty EM, Dominguez C, Gavva NR, Gore V, Ma V, Nishimura N, Surapaneni S, Tang P, Tamir R, Thiel O, Treanor JJ, Norman MH.

J Med Chem. 2007 Jul 26;50(15):3528-39. Epub 2007 Jun 22.

PMID:
17585751
6.

Design, synthesis, and biological evaluation of novel diarylalkyl amides as TRPV1 antagonists.

Li FN, Kim NJ, Paek SM, Kwon DY, Min KH, Jeong YS, Kim SY, Park YH, Kim HD, Park HG, Suh YG.

Bioorg Med Chem. 2009 May 15;17(10):3557-67. doi: 10.1016/j.bmc.2009.04.010. Epub 2009 Apr 11.

PMID:
19398205
7.

TRPV1 receptors in the CNS play a key role in broad-spectrum analgesia of TRPV1 antagonists.

Cui M, Honore P, Zhong C, Gauvin D, Mikusa J, Hernandez G, Chandran P, Gomtsyan A, Brown B, Bayburt EK, Marsh K, Bianchi B, McDonald H, Niforatos W, Neelands TR, Moreland RB, Decker MW, Lee CH, Sullivan JP, Faltynek CR.

J Neurosci. 2006 Sep 13;26(37):9385-93.

8.

Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.

Ratcliffe P, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, Maclean J, McArthur D, McGregor D, McLuskey H, Neagu I, Nimz O, Nisbet LA, Ohlmeyer M, Palin R, Pham Q, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G.

Bioorg Med Chem Lett. 2011 Aug 1;21(15):4652-7. doi: 10.1016/j.bmcl.2011.01.051. Epub 2011 Jan 26.

PMID:
21723725
9.

Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.

Doherty EM, Fotsch C, Bannon AW, Bo Y, Chen N, Dominguez C, Falsey J, Gavva NR, Katon J, Nixey T, Ognyanov VI, Pettus L, Rzasa RM, Stec M, Surapaneni S, Tamir R, Zhu J, Treanor JJ, Norman MH.

J Med Chem. 2007 Jul 26;50(15):3515-27. Epub 2007 Jun 22.

PMID:
17585750
10.

Synthesis of Analogues of BCTC Incorporating a Pyrrolidinyl Linker and Biological Evaluation as Transient Receptor Potential Vanilloid 1 Antagonists.

Yan L, Wang J, Pan M, Qiu Q, Huang W, Qian H.

Chem Biol Drug Des. 2016 Feb;87(2):306-11. doi: 10.1111/cbdd.12661. Epub 2015 Oct 5.

PMID:
26360809
11.

Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists.

Li FN, Kim NJ, Chang DJ, Jang J, Jang H, Jung JW, Min KH, Jeong YS, Kim SY, Park YH, Kim HD, Park HG, Suh YG.

Bioorg Med Chem. 2009 Dec 15;17(24):8149-60. doi: 10.1016/j.bmc.2009.10.043. Epub 2009 Oct 27.

PMID:
19897373
12.

Additive antinociceptive effects of the selective Nav1.8 blocker A-803467 and selective TRPV1 antagonists in rat inflammatory and neuropathic pain models.

Joshi SK, Honore P, Hernandez G, Schmidt R, Gomtsyan A, Scanio M, Kort M, Jarvis MF.

J Pain. 2009 Mar;10(3):306-15. doi: 10.1016/j.jpain.2008.09.007. Epub 2008 Dec 13.

PMID:
19070548
13.

Synthesis of oxazolo[4,5-c]quinoline TRPV1 antagonists.

Voight EA, Daanen JF, Kort ME.

J Org Chem. 2010 Dec 17;75(24):8713-5. doi: 10.1021/jo101938b. Epub 2010 Nov 23.

PMID:
21090730
14.

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.

Bioorg Med Chem. 2012 Jan 1;20(1):215-24. doi: 10.1016/j.bmc.2011.11.008. Epub 2011 Nov 22.

15.

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.

Bioorg Med Chem Lett. 2005 Sep 15;15(18):4143-50.

PMID:
15993063
16.

Potent and orally efficacious benzothiazole amides as TRPV1 antagonists.

Besidski Y, Brown W, Bylund J, Dabrowski M, Dautrey S, Harter M, Horoszok L, Hu Y, Johnson D, Johnstone S, Jones P, Leclerc S, Kolmodin K, Kers I, Labarre M, Labrecque D, Laird J, Lundström T, Martino J, Maudet M, Munro A, Nylöf M, Penwell A, Rotticci D, Slaitas A, Sundgren-Andersson A, Svensson M, Terp G, Villanueva H, Walpole C, Zemribo R, Griffin AM.

Bioorg Med Chem Lett. 2012 Oct 1;22(19):6205-11. doi: 10.1016/j.bmcl.2012.08.018. Epub 2012 Aug 14.

PMID:
22939234
17.

Design of potent, orally available antagonists of the transient receptor potential vanilloid 1. Structure-activity relationships of 2-piperazin-1-yl-1H-benzimidazoles.

Ognyanov VI, Balan C, Bannon AW, Bo Y, Dominguez C, Fotsch C, Gore VK, Klionsky L, Ma VV, Qian YX, Tamir R, Wang X, Xi N, Xu S, Zhu D, Gavva NR, Treanor JJ, Norman MH.

J Med Chem. 2006 Jun 15;49(12):3719-42.

PMID:
16759115
18.
19.

Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.

Palin R, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Maclean J, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, McArthur D, McGregor D, McLuskey H, Neagu I, Neale S, Nisbet LA, Ohlmeyer M, Pham Q, Ratcliffe P, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):892-8. doi: 10.1016/j.bmcl.2010.12.092. Epub 2010 Dec 23.

PMID:
21236666
20.

Dopamides, vanillylamides, ethanolamides, and arachidonic acid amides of anti-inflammatory and analgesic drug substances as TRPV1 ligands.

Sinning C, Watzer B, De Petrocellis L, Di Marzo V, Imming P.

ChemMedChem. 2008 Dec;3(12):1956-64. doi: 10.1002/cmdc.200800271.

PMID:
19003845

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