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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

Title
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 N.-J.Li F.-N.Lee J.H.Park S.-G.Kim K.Lim C.Han Y.T.Yun H.Jung J.-W.Park H.-G.Kim H.-D.Woo B.Y.Shin S.S.Kim S.-Y.Choi J.K.Jeong Y.-S.Park Y.Park Y.-H.Kim D.-D.Choi S.Suh Y.-G.
Ewha Authors
최선
SCOPUS Author ID
최선scopus
Issue Date
2013
Journal Title
Chemistry - An Asian Journal
ISSN
1861-4728JCR Link
Citation
vol. 8, no. 2, pp. 400 - 409
Indexed
SCI; SCIE; SCOPUS WOS scopus
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. Flexibility not desired: 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. Copyright © 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
DOI
10.1002/asia.201200730
Appears in Collections:
약학대학 > 약학과 > Journal papers
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