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

J Lee, SU Kang, MJ Kil, M Shin, JO Lim, HK Choi…

Index: Lee, Jeewoo; Kang, Sang-Uk; Kil, Min-Jung; Shin, Myoungyoup; Lim, Ju-Ok; Choi, Hyun-Kyung; Jin, Mi-Kyoung; Kim, Su Yeon; Kim, Sung-Eun; Lee, Yong-Sil; Min, Kyung-Hoon; Kim, Young-Ho; Ha, Hee-Jin; Tran, Richard; Welter, Jacqueline D.; Wang, Yun; Szabo, Tamas; Pearce, Larry V.; Lundberg, Daniel J.; Toth, Attila; Pavlyukovets, Vladimir A.; Morgan, Matthew A.; Blumberg, Peter M. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 18 p. 4136 - 4142

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Citation Number: 23

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.