Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio) amides as novel TRPV1 antagonists

…, NJ Kim, DJ Chang, J Jang, H Jang, JW Jung…

Index: Li, Fu-Nan; Kim, Nam-Jung; Chang, Dong-Jo; Jang, Jaebong; Jang, Hannah; Jung, Jong-Wha; Min, Kyung-Hoon; Jeong, Yeon-Su; Kim, Sun-Young; Park, Young-Ho; Kim, Hee-Doo; Park, Hyeung-Geun; Suh, Young-Ger Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 24 p. 8149 - 8160

Full Text: HTML

Citation Number: 5

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 ...