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

J Lee, MK Jin, SU Kang, SY Kim, J Lee, M Shin…

Index: Lee, Jeewoo; Jin, Mi-Kyoung; Kang, Sang-Uk; Su, Yeon Kim; Lee, Jiyoun; Shin, Myoungyoup; Hwang, Jaemin; Cho, Sookhyun; Choi, Yeon-Sil; Choi, Hyun-Kyung; Kim, Sung-Eun; Suh, Young-Ger; Lee, Yong-Sil; Kim, Young-Ho; Ha, Hee-Jin; Toth, Attila; Pearce, Larry V.; Tran, Richard; Szabo, Tamas; Welter, Jacqueline D.; Lundberg, Daniel J.; Wang, Yun; Lazar, Jozsef; Pavlyukovets, Vladimir A.; Morgan, Matthew A.; Blumberg, Peter M. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 18 p. 4143 - 4150

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Citation Number: 16

Abstract

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.