Conformationally constrained analogues of N'-(4-tert-butylbenzyl)-N-(4-methylsulfonylaminobenzyl)thiourea as TRPV1 antagonists |
| |
Authors: | Lim Ju-Ok Jin Mi-Kyoung Ryu HyungChul Kang Dong Wook Lee Jeewoo Pearce Larry V Tran Richard Toth Attila Blumberg Peter M |
| |
Affiliation: | Laboratory of Medicinal Chemistry, Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Shinlim-Dong, Kwanak-Ku, Seoul 151-742, Republic of Korea. |
| |
Abstract: | A series of bicyclic analogues having indan and tetrahydronaphthalene templates in the A-region were designed as conformationally constrained analogues of our previously reported potent TRPV1 antagonists (1, 3). The activities for rat TRPV1 of the conformationally restricted analogues were moderately or markedly diminished, particularly in the case of the tetrahydronaphthalene analogues. The analysis indicated that steric constraints at the benzylic position in the bicyclic analogues may be an important factor for their unfavorable interaction with the receptor. |
| |
Keywords: | |
本文献已被 PubMed 等数据库收录! |
|