Literature DB >> 16005215

Analysis of structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues as TRPV1 antagonists.

Jeewoo Lee1, Sang-Uk Kang, Min-Jung Kil, Myoungyoup Shin, Ju-Ok Lim, Hyun-Kyung Choi, Mi-Kyoung Jin, Su Yeon Kim, Sung-Eun Kim, Yong-Sil Lee, Kyung-Hoon Min, Young-Ho Kim, Hee-Jin Ha, Richard Tran, Jacqueline D Welter, Yun Wang, Tamas Szabo, Larry V Pearce, Daniel J Lundberg, Attila Toth, Vladimir A Pavlyukovets, Matthew A Morgan, Peter M Blumberg.   

Abstract

The structure-activity relationships for the 'A-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. The 2-halogen analogues showed enhanced antagonism compared to the prototype antagonist.

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Year:  2005        PMID： 16005215     DOI： 10.1016/j.bmcl.2005.06.009

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  5 in total

1.  Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists.

Authors:  Ju-Ok Lim; Mi-Kyoung Jin; HyungChul Ryu; Dong Wook Kang; Jeewoo Lee; Larry V Pearce; Richard Tran; Attila Toth; Peter M Blumberg
Journal:  Eur J Med Chem       Date:  2008-03-07       Impact factor: 6.514

2.  Halogenation of 4-hydroxy/amino-3-methoxyphenyl acetamide TRPV1 agonists showed enhanced antagonism to capsaicin.

Authors:  Dong Wook Kang; Yong Soo Kim; Kwang Su Lim; Myeong Seop Kim; Larry V Pearce; Vladimir A Pavlyukovets; Andy K Tao; Krystle A Lang-Kuhs; Peter M Blumberg; Jeewoo Lee
Journal:  Bioorg Med Chem       Date:  2010-09-18       Impact factor: 3.641

3.  Design, synthesis, insecticidal activity, and structure-activity relationship (SAR): studies of novel triazone derivatives containing a urea bridge group based on transient receptor potential (TRP) channels.

Authors:  Yan Yang; Yuxiu Liu; Hongjian Song; Yongqiang Li; Qingmin Wang
Journal:  Mol Divers       Date:  2016-07-06       Impact factor: 2.943

4.  The SAR analysis of TRPV1 agonists with the α-methylated B-region.

Authors:  Yongsung Cho; Myeong Seop Kim; Ho Shin Kim; Jihyae Ann; Jiyoun Lee; Larry V Pearce; Vladimir A Pavlyukovets; Matthew A Morgan; Peter M Blumberg; Jeewoo Lee
Journal:  Bioorg Med Chem Lett       Date:  2012-06-23       Impact factor: 2.823

5.  Novel scaffolds for modulation of TRPV1 identified with pharmacophore modeling and virtual screening.

Authors:  Daria Goldmann; Peter Pakfeifer; Steffen Hering; Gerhard F Ecker
Journal:  Future Med Chem       Date:  2015       Impact factor: 4.767
  5 in total

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