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

Bioorganic & medicinal chemistry letters 2005 Sep 15; 15(18):4136-42

Link to PubMed abstract

Lee J J, Kang S SU, Kil M MJ, Shin M M, Lim J JO, Choi H HK, Jin M MK, Kim S SY, Kim S SE, Lee Y YS, Min K KH, Kim Y YH, Ha H HJ, Tran R R, Welter J JD, Wang Y Y, Szabo T T, Pearce L LV, Lundberg D DJ, Toth A A, 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 '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.