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Heterocycle-linked Phenylbenzyl Amides as Novel TRPV1 Antagonists and Their TRPV1 Binding Modes: Constraint-Induced Enhancement of In Vitro and In Vivo Activities
- Authors
- Kim, Nam-Jung; Li, Fu-Nan; Lee, Jin Hee; Park, Seul-gi; Kim, Kyeojin; Lim, Changjin; Han, Young Taek; Yun, Hwayoung; Jung, Jong-Wha; Park, Hyeung-geun; Kim, Hee-Doo; Woo, Byoung Young; Shin, Song Seok; Kim, Sun-Young; Choi, Jin Kyu; Jeong, Yeon-Su; Park, Yanghui; Park, Young-Ho; Kim, Dae-Duk; Choi, Sun; Suh, Young-Ger
- Issue Date
- Feb-2013
- Publisher
- WILEY-V C H VERLAG GMBH
- Keywords
- antagonists; ligand design; medicinal chemistry; molecular modeling; TRVP1
- Citation
- CHEMISTRY-AN ASIAN JOURNAL, v.8, no.2, pp 400 - 409
- Pages
- 10
- Journal Title
- CHEMISTRY-AN ASIAN JOURNAL
- Volume
- 8
- Number
- 2
- Start Page
- 400
- End Page
- 409
- ISSN
- 1861-4728
1861-471X
- Abstract
- A series of heterocycle-linked constrained phenylbenzyl amides were found to be TRPV1 antagonists with promising in vivo profiles. In particular, one of the analogues containing a furan linker exhibited excellent TRPV1 antagonistic activity and in vivo analgesic efficacy. In addition, the binding modes of dibenzyl thiourea, benzylphenethyl amide, and furan-linked phenylbenzyl amide were examined by using the flexible docking study within the rTRPV1 homology model.
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