Title of article
Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists Original Research Article
Author/Authors
Structural optimization of multiple H-bonding region and structure–activity relationship of diarylalkyl amides/thioamides as novel TRPV1 antagonists are described. In particular، نويسنده , , we identified amide 34o and thioamides 35o and 35r، نويسنده , , of which antagonistic activities were highly enhanced by an incorporation of cyano or vinyl-substituent to the multiple H-bonding region. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron with IC50s of 25، نويسنده , , 32 and 28 nM، نويسنده , , respectively.، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2009
Pages
12
From page
8149
To page
8160
Abstract
Structural optimization of multiple H-bonding region and structure–activity relationship of diarylalkyl amides/thioamides as novel TRPV1 antagonists are described. In particular, we identified amide 34o and thioamides 35o and 35r, of which antagonistic activities were highly enhanced by an incorporation of cyano or vinyl-substituent to the multiple H-bonding region. They exhibited potent 45Ca2+ uptake inhibitions in rat DRG neuron with IC50s of 25, 32 and 28 nM, respectively.
Journal title
Bioorganic and Medicinal Chemistry
Serial Year
2009
Journal title
Bioorganic and Medicinal Chemistry
Record number
1306599
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