Synthesis and structural optimization of multiple H-bonding region of diarylalkyl (thio)amides as novel TRPV1 antagonists |
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| Authors: | Fu-Nan Li Nam-Jung Kim Dong-Jo Chang Jaebong Jang Hannah Jang Jong-Wha Jung Kyung-Hoon Min Yeon-Su Jeong Sun-Young Kim Young-Ho Park Hee-Doo Kim Hyeung-Geun Park Young-Ger Suh |
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| Affiliation: | 1. College of Pharmacy, Seoul National University, 599 Gwanak-ro, Gwanak-gu, Seoul 151-742, Republic of Korea;2. College of Pharmacy, Chung-Ang University, Heukseok-dong, Dongjak-gu, Seoul 156-756, Republic of Korea;3. Amorepacific R&D Center 314-1, Bora-dong, Giheung-gu, Yongin-si, Gyeonggi-do 446-729, Republic of Korea;4. College of Pharmacy, Sookmyung women’s University, 52 Hyochangwon-Gil, Yongsan-gu, Seoul 140-742, Republic of Korea |
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| 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. |
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