Design, synthesis and biological evaluation of B-region modified diarylalkyl amide analogues as novel TRPV1 antagonists
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, h...
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Published in | Archives of pharmacal research Vol. 37; no. 4; pp. 440 - 451 |
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Main Authors | , , , |
Format | Journal Article |
Language | Korean |
Published |
2014
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Subjects | |
Online Access | Get full text |
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Summary: | 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 ${\alpha}$-substituted acetamides were introduced at the B-region. TRPV1 antagonistic activities of these analogues were evaluated by $^{45}Ca^{2+}$ uptake assay in rat DRG neuron. In particular, ${\alpha},{\alpha}$-difluoroamide 53 exhibited 3-fold more potent TRPV1 antagonistic activity ($IC_{50}=0.058{\mu}M$) than the parent amide analogue 6. |
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Bibliography: | KISTI1.1003/JNL.JAKO201426955812275 |
ISSN: | 0253-6269 1976-3786 |