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

Research output: Contribution to journalArticle

15 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)447-450
Number of pages4
JournalOrganic and Biomolecular Chemistry
Volume6
Issue number3
DOIs
Publication statusPublished - 2008 Feb 1
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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  • Cite this

    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