Analysis of structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]-thiourea analogues as TRPV1 antagonists.
Bioorganic & medicinal chemistry letters 2005 Sep 15; 15(18):4143-50
Lee J J, Jin M MK, Kang S SU, Kim S SY, Lee J J, Shin M M, Hwang J J, Cho S S, Choi Y YS, Choi H HK, Kim S SE, Suh Y YG, Lee Y YS, Kim Y YH, Ha H HJ, Toth A A, Pearce L LV, Tran R R, Szabo T T, Welter J JD, Lundberg D DJ, Wang Y Y, Lazar J J, Pavlyukovets V VA, Morgan M MA, Blumberg P PM
Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151-742, Republic of Korea. jeewoo@snu.ac.kr
The structure-activity relationships for the 'B-region' of N-(4-t-butylbenzyl)-N'-[4-(methylsulfonylamino)benzyl]thiourea analogues have been investigated as TRPV1 receptor antagonists. A docking model of potent antagonist 2 with the sensor region of TRPV1 is proposed.