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KMID : 0043320140370040440
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Archives of Pharmacal Research
2014 Volume.37 No. 4 p.440 ~ p.451
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Design, synthesis and biological evaluation of B-region modified diarylalkyl amide analogues as novel TRPV1 antagonists
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Han Young-Taek
Yang Shao Mei
Wang Xiao Yuan
Li Fu Nan
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Abstract
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Design, synthesis and biological evaluation of B-region, known to be a dipolar interacting pharmacophore, modified diarylalkyl amide analogues for novel TRPV1 (transient receptor potential channel, vanilloid subfamily member 1) antagonists was described. A variety of moieties including guanidines, heterocyclic rings, cinnamides, and α-substituted acetamides were introduced at the B-region. TRPV1 antagonistic activities of these analogues were evaluated by 45Ca2+ uptake assay in rat DRG neuron. In particular, α,α-difluoroamide 53 exhibited 3-fold more potent TRPV1 antagonistic activity (IC50 = 0.058 μM) than the parent amide analogue 6.
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KEYWORD
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TRPV1, TRPV1 antagonist, Structural modification, Diarylalkyl amide analogues
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