Structure–activity relationships of simplified resiniferatoxin analogues with potent VR1 agonism elucidates an active conformation of RTX for VR1 binding

…, SU Kang, HK Choi, MK Jin, JD Welter, T Szabo…

文献索引：Lee, Jeewoo; Kim, Su Yeon; Park, Soyoung; Lim, Ju-Ok; Kim, Ji-Min; Kang, Myungshim; Lee, Jiyoun; Kang, Sang-Uk; Choi, Hyun-Kyung; Jin, Mi-Kyung; Welter, Jacqueline D.; Szabo, Tamas; Tran, Richard; Pearce, Larry V.; Toth, Attila; Blumberg, Peter M. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 5 p. 1055 - 1069

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被引用次数: 14

摘要

We previously described a series of N-(3-acyloxy-2-benzylpropyl) homovanillate and N′-(4- hydroxy-3-methoxybenzyl) thiourea derivatives that were potent VR1 agonists with high- affinities and excellent analgesic profiles. The design of these simplified RTX analogues was based on our RTX-derived pharmacophore model which incorporates the 4-hydroxy-3- methoxyphenyl (A-region), C20-ester (B-region), orthophenyl (C1-region) and C3-keto ( ...