Design, synthesis, and biological evaluation of novel alkenylthiophenes as potent and selective CB1 cannabinoid receptor antagonists

Chia Liang Tai, Ming Shiu Hung, Vijay D. Pawar, Shi Liang Tseng, Jen Shin Song, Wan Ping Hsieh, Hua Hao Chiu, Hui Chuan Wu, Min Tsang Hsieh, Chun Wei Kuo, Chia Chien Hsieh, Jing Po Tsao, Yu Sheng Chao, Kak Shan Shia

研究成果: 雜誌貢獻文章

15 引文 斯高帕斯(Scopus)

摘要

A novel class of (5-(pent-1-enyl)thiophen-2-yl)pyrazole antagonists was discovered, many of which exhibited potent CB1 activity and good CB1/2 selectivity, suggesting that along with a 1,3-transposition of the carbonyl of the pyrazole 3-carboxamide, bioisosteric replacement of the conventional pyrazole 5-aryl group with a thienyl ring substituted with an appropriate alkenyl moiety is viable.

原文英語
頁(從 - 到)447-450
頁數4
期刊Organic and Biomolecular Chemistry
6
發行號3
DOIs
出版狀態已發佈 - 2008 二月 1
對外發佈Yes

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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    Tai, C. L., Hung, M. S., Pawar, V. D., Tseng, S. L., Song, J. S., Hsieh, W. P., Chiu, H. H., Wu, H. C., Hsieh, M. T., Kuo, C. W., Hsieh, C. C., Tsao, J. P., Chao, Y. S., & Shia, K. S. (2008). Design, synthesis, and biological evaluation of novel alkenylthiophenes as potent and selective CB1 cannabinoid receptor antagonists. Organic and Biomolecular Chemistry, 6(3), 447-450. https://doi.org/10.1039/b716434c